WO2001064177A1 - Use of flavones or isoflavones for the treatment of cellulite - Google Patents

Use of flavones or isoflavones for the treatment of cellulite

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Publication number
WO2001064177A1
WO2001064177A1 PCT/EP2001/002070 EP0102070W WO0164177A1 WO 2001064177 A1 WO2001064177 A1 WO 2001064177A1 EP 0102070 W EP0102070 W EP 0102070W WO 0164177 A1 WO0164177 A1 WO 0164177A1
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WO
WIPO (PCT)
Prior art keywords
acid
use according
preparation
substances
cellulite
Prior art date
Application number
PCT/EP2001/002070
Other languages
German (de)
French (fr)
Inventor
Ulrich Issberner
Marcus Claas
Vera Maienschein
Silke Nieveler
Thomas Förster
Werner Köhl
Original Assignee
Henkel Kommanditgesellschaft Auf Aktien
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Henkel Kommanditgesellschaft Auf Aktien filed Critical Henkel Kommanditgesellschaft Auf Aktien
Priority to AU2001246471A priority Critical patent/AU2001246471A1/en
Priority to EP01919334A priority patent/EP1259221A1/en
Publication of WO2001064177A1 publication Critical patent/WO2001064177A1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4973Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • A61K8/498Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/42Amides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A61K8/4953Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom containing pyrimidine ring derivatives, e.g. minoxidil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • A61K8/602Glycosides, e.g. rutin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/06Preparations for care of the skin for countering cellulitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74Biological properties of particular ingredients
    • A61K2800/78Enzyme modulators, e.g. Enzyme agonists
    • A61K2800/782Enzyme inhibitors; Enzyme antagonists

Definitions

  • the invention relates to the use of a composition comprising a flavone, isoflavone or a glycoside thereof and optionally a substance that stimulates and / or depolarizes the C-nerve fibers for the cosmetic or pharmaceutical treatment of cellulite.
  • Cellulite (synonyms: panniculosis, lipodystrophy, status protrusis cutis, orange peel) is a local accumulation of fat and water in body tissue. It is a predominantly aesthetic problem associated with pitting and deepening of the skin and nodulation of the subcutaneous fatty tissue, particularly on the thighs and buttocks. In the context of the present invention, local fat excess weights are also included under the term cellulite. In advanced stages of cellulite, pain in the area of the nodules can also occur. A clear distinction from cellulite is cellulitis (panniculitis), which is an inflammation of the subcutaneous adipose tissue and thus a serious and life-threatening illness in some cases.
  • panniculitis panniculitis
  • the conventional treatment methods for cellulite try to promote blood circulation and have a positive influence on the connective tissue structure, for example through
  • the best known and most widespread of the methods of stimulating lipolysis is to inhibit the enzyme phosphodiesterase in order to prevent or at least slow down the degradation of the cyclic AMP.
  • the phosphodiesterase destroys the cyclic AMP by converting it to 5 ' -AMP, which is no longer able to activate lipolysis. It is therefore important to inhibit the action of the phosphodiesterase in such a way that a high concentration of cyclic AMP is achieved in the region of the adipocytes with the aim of stimulating lipolysis.
  • various phosphodiesterase inhibitors that have been recommended, for example, as slimming agents, are the xanthine bases, especially caffeine.
  • FR 2740681 describes cosmetic compositions for the treatment of cellulite which contain caffeine and an extract from the bark or leaves of plants of the genus Viburnum.
  • Amentoflavon a biflavonoid consisting of two apigenin units, is described as a component of this extract.
  • amentoflavone is a characteristic ingredient of viburnum and serves to standardize the dosage of the viburnum extract in the compositions according to the invention. The document does not give the person skilled in the art any indication that the amentoflavone could be the cause or jointly responsible for the anti-cellulite effect of the compositions.
  • compositions with a local slimming effect which is attributed to their intracellular phosphodiesterase-inhibiting action.
  • the compositions may contain glycosides such as bioflavonoids as additional ingredients. It is not disclosed which substances or groups of substances are to be understood under the term bioflavonoids, which is known to be contradictory in the specialist world. This does not enable the person skilled in the art to prepare a composition according to the teaching of the writing containing a bioflavonoid which has a locally slimming effect. The document also gives no indication that the bioflavonoids could contribute to the slimming properties of the compositions according to the invention.
  • the object of the invention was to remedy the shortcomings of the prior art and to provide improved agents for treating cellulite.
  • the object of the invention is achieved by the use of a composition comprising a flavone, isoflavone or their glycoside and optionally a substance which stimulates and / or depolarizes carbon nerve fibers, for the cosmetic treatment of cellulite or for firming the skin.
  • the invention accordingly furthermore relates to the use of a composition comprising a flavone, isoflavone or their glycoside and, if appropriate, a substance which stimulates and / or depolarizes C-nerve fibers, for the production of a pharmaceutical preparation for the therapeutic treatment of cellulite.
  • flavones are understood to mean substances which are hydrogenation, oxidation or substitution products of 2-phenyl-4H-1-benzopyran, where hydrogenation can be present in the 2,3-position of the carbon skeleton, oxidation under Formation of a carbonyl group may be in the 4-position, and substitution is to be understood as the replacement of one or more hydrogen atoms by hydroxyl or methoxy groups.
  • This definition therefore includes flavans, flavan-3-oles (catechins), flavan-3,4-diols (leucoanthocyanidins), flavones, flavonols and flavanones in the conventional sense.
  • the flavones according to the invention include, for example, chrysin, galangin, apigenin, fisetin, luteolin, camphor oil, quercetin, Mon, Robinetin, Gossypetin, Taxifolin, Myricetin, Rhamnetin, Isorhamnetin, Naringenin, Eriodyctiol, Hesperetin, Liquiritigenin, Catechin and Epicatechin. Quercetin and luteolin are preferred as flavones.
  • the flavones are glycosidically linked to at least one sugar via at least one hydroxyl group.
  • Monosaccharides and oligosaccharides in particular D-glucose, D-galactose, D-glucuronic acid, D-galacturonic acid, D-xylose, D-apiose, L-rhamnose, L-arabinose and rutinose are suitable as sugars.
  • Examples of the flavone glycosides according to the invention are rutin, hesperidin and naringin.
  • isoflavones are understood to mean substances which are hydrogenation, oxidation or substitution products of 3-phenyl-4H-1-benzopyran, where hydrogenation can be present in the 2,3-position of the carbon skeleton, oxidation under Formation of a carbonyl group may be in the 4-position, and substitution is to be understood as the replacement of one or more hydrogen atoms by hydroxyl or methoxy groups.
  • the isoflavones according to the invention include, for example, daidzein, genistein, prunetin, biochanin, Orobol, Santal, pratensein, irigenin, glycitein, biochanin A and formononetin. Daidzein, genistein, glycitein and formononetin are preferred as isoflavones.
  • the isoflavones are glycosidically linked to at least one sugar via at least one hydroxyl group.
  • Suitable sugars are mono- or oligosaccharides, in particular D-glucose, D-galactose, D-glucuronic acid, D-galacturonic acid, D-xylose, D-apiose, L-rhamnose, L-arabinose and rutinose.
  • Preferred examples of the isoflavone glycosides according to the invention are daidzin and genistin.
  • the C-nerve fibers also called polymodal C-nerve fibers, play an important role in the human organism for the sensory functions of the body, especially the skin. They are primarily perception for example from warmth, cold and itching as well as the sensation of pain (e.g. heat pain, cold pain, stinging pain, burning pain).
  • the polymodal C-nerve fibers have a special position as a sub-group of the C-nerve fibers because they can react to several different stimuli and can also intervene in the stimulus process through the release of mediators.
  • Different receptors such as capsaicin, bradykinin and 5-hydroxytryptamine receptors are located on the surface of the C-nerve fibers, as well as ion channels such as calcium and sodium channels, via which the C-nerve fibers can be stimulated and / or depolarized.
  • This stimulation and / or depolarization triggers a sensory stimulus which manifests itself, for example, as a burning sensation, tingling sensation, warmth, coldness or pain.
  • it is preferred to trigger a tingling sensation, a slight burning sensation or a feeling of warmth or coldness by stimulating and / or depolarizing the C-nerve fibers of the skin, in particular by stimulating the capsaicin receptors of these nerve fibers.
  • substances influencing C nerve fibers are to be understood, for example:
  • Preferred substances influencing C-nerve fibers are capsaicin, N-vanillyl nonanamide and their glycosides.
  • An advantage of the preparations according to the invention with substances that stimulate and / or depolarize C-nerve fibers is the generation of a physiological and / or psychological effect which is independent of the treatment effect on cellulite and which the user already has immediately during or after the application of the agent gives a subjective impression of an onset of effect.
  • the improvement in cellulite by the preparations according to the invention is achieved in particular by the breakdown of fat cells and the remodeling of connective tissue, which is why the success of the treatment becomes visible only after prolonged use due to physiological reasons. In practice, however, it has been shown that the users of an anti-cellulite agent very soon stop using the agent and are disappointed with the product used if they do not at least have the subjective impression that the agent has an effect.
  • the presence of substances which stimulate and / or depolarize C-nerve fibers triggers a sensible stimulus in the user, which subjectively gives him an impression of the effect.
  • the substances that influence the C-nerve fibers sometimes have other desired effects. They promote the blood flow to the treated tissue and thus promote the penetration of the ingredients of the preparation into the skin. Furthermore, the removal of the degradation products which arise in the course of the lipolysis which is brought about by the use of the preparation can be promoted. In addition, cellulite in severe cases Pain be dampened. This is the case, for example, when nonivamide (N-vanillyl-nonanamide) is used as the substance influencing the C-nerve fibers.
  • the active substances are used according to the invention in concentrations such that the toxicologically permissible use concentration in preparations or during use is not exceeded.
  • the preparations contain the flavones, isoflavones and their glycosides as constituents of a mixture of substances obtained from a plant, in particular a plant extract.
  • a plant extract obtained from a plant, in particular a plant extract.
  • Such vegetable substance mixtures can be obtained in a manner familiar to the person skilled in the art, for example by pressing or extracting them from plants such as soybean, red clover or chickpeas.
  • Isoflavones or isoflavone glycosides in the form of extracts obtained from soy are particularly preferably used in the preparations according to the invention, such as those known under the product name Soy Protein Isolate SPI (Protein Technology International, St. Louis) or Soy Phytochemicals Concentrate SPC (Archer Daniels Midland, Decatur) are commercially available.
  • Alcohols and mixtures thereof can be used.
  • the alcohols are lower alcohols such as especially ethanol and isopropanol, and polyvalent ones
  • Alcohols such as ethylene glycol, propylene glycol and butylene glycol, both as the sole extracting agent and in a mixture with water, are preferred.
  • Alcoholic extraction is preferred according to the invention.
  • the invention relates to the use of a composition comprising a flavone, isoflavone or their glycoside and, if appropriate, a substance which stimulates and / or depolarizes C-nerve fibers, in combination with a phosphodiesterase inhibitor for the cosmetic treatment of cellulite or for the preparation a pharmaceutical preparation for the therapeutic treatment of cellulite.
  • suitable phosphodiesterase inhibitors are, for example, inhibitors as described in RM Di Salvo, Controlling the Appearance of Cellulite, Cosmetics and Toiletries Magazine 110, pp. 50-59 (1995) or in L. Stryer, Biochemie, Spektrum Akademischer Verlag GmbH, Heidelberg 1991, p. 482.
  • xanthine or a methylxanthine are preferably considered as phosphodiesterase inhibitors, methyl xanthine being a xanthine derivative in which one or more hydrogen atoms are replaced by methyl groups.
  • Theophylline, theobromine and caffeine are preferred as methylxanthines, and caffeine is particularly preferred.
  • the cosmetic or pharmaceutical preparations contain a total of 0.1 to 20% by weight, and preferably 1 to 10% by weight, of one or more flavones, isoflavones or their glycosides and optionally 0.0001 to 3% by weight and preferably 0.005 to 0.5% by weight of one or more substances which stimulate and / or depolarize the C nerve fibers, based on the total weight of the preparation.
  • the cosmetic or pharmaceutical preparations additionally contain a total of 1 to 15% by weight, and preferably 5 to 10% by weight, of one or more phosphodiesterase inhibitors, based on the total weight of the preparation.
  • the combination according to the invention consists of
  • the cosmetic or pharmaceutical preparations contain
  • composition comprising a flavone, isoflavone or their glycoside and optionally a substance which stimulates and / or depolarizes C-nerve fibers, is preferably carried out together with a physiologically tolerable carrier in the form of a cosmetic preparation.
  • the physiologically acceptable carrier of the cosmetic or pharmaceutical preparations comprises one or more adjuvants, as are usually used in such preparations, such as.
  • adjuvants such as.
  • Electrolytes Sequestrants organic solvents, preservatives, bactericides, antioxidants, vitamins, fragrances, flavors, sweeteners, colors and pigments.
  • the cosmetic and pharmaceutical preparations according to the invention are advantageously in the form of a liquid or solid oil-in-water emulsion, water-in-oil emulsion, multiple emulsion, microemulsion, PIT emulsion or Pickering emulsion, a hydrogel, an alcoholic gel, a lipogel, a single or multi-phase solution, a foam, an ointment, a plaster, a suspension, a powder or a mixture with at least one polymer suitable as a medical adhesive.
  • the skin treatment compositions according to the invention can also be administered in anhydrous form, such as, for example, an oil or a balm.
  • the carrier can be a vegetable or animal oil, a mineral oil, a synthetic oil or a mixture of such oils.
  • microemulsions are understood to mean not only the thermodynamically stable microemulsions but also the so-called “PIT” emulsions.
  • PIT phase inversion temperature
  • O / W emulsions are again formed, but these are also present at room temperature as microemulsions or as very fine-particle emulsions with an average particle diameter below 400 nm and in particular from about 100-300 nm.
  • those micro- or "PIT" emulsions can be preferred which have an average particle diameter of approximately 200 nm. Details regarding these "PIT emulsions” e.g. B. the publication Angew. Chem. 97, 655-669 (1985).
  • the pharmaceutical preparations according to the invention are also administered enterally, parenterally or rectally.
  • the pharmaceutical preparations can be in the form of tablets, capsules, dragees, syrups, suspensions, solutions, powders, granules or emulsions.
  • the preparations may be in the form of solutions or suspensions for perfusion or injection.
  • the preparations can be in the form of suppositories for administration by the rectal route.
  • Suitable fat substances are for example:
  • vegetable oils such as sunflower oil, olive oil, soybean oil, rapeseed oil, almond oil, jojoba oil, orange oil, wheat germ oil, peach seed oil and the liquid components of coconut oil,
  • paraffin oils e.g. 1, 3-di- (2-ethyl-hexyl) cyclohexane (Cetiol ® S) or polydecene,
  • Di-n-alkyl ethers with a total of 12 to 36, in particular 12 to 24 carbon atoms, for.
  • di-n-octyl ether (Cetiol ® OE)
  • di-n-n-hexyl-n-octyl ether di-n-octyl-n-decyl ether.
  • C 8 - 3 o-fatty acids especially linear and / or branched, saturated and / or unsaturated C 8 - 3 o-fatty acids.
  • C ⁇ o- 22 fatty acids are preferred. Examples are the isostearic acids and isopalmitic acids such as the fatty acids sold under the trade name Edenor ® .
  • fatty acids are caproic acid, caprylic acid, 2-ethylhexanoic acid, capric acid, lauric acid, isotridecanoic acid, myristic acid, palmitic acid, palmitoleic acid, stearic acid, isostearic acid, oleic acid, elaidic acid, petroselinic acid, linoleic acid, linolenic acid, arenachidonic acid, gadachoic acid, gadachoic acid, gadolinic acid, gadachoic acid, gadachoic acid, gadachic acid, gaurachidic acid, gadic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic
  • the fatty acid cuts that are obtainable from coconut oil or palm oil are usually particularly preferred; the use of stearic acid is particularly preferred.
  • Esteröle that is, esters of C 6 - 3 o-fatty acids with C. 2 30 fatty alcohols.
  • the monoesters of fatty acids with alcohols having 2 to 24 carbon atoms are preferred.
  • the above-mentioned substances can be used as alcohol and acid components of the ester oils.
  • Hydroxycarboxylic acid alkyl esters wherein the Vollester of glycolic acid, lactic acid, malic acid, tartaric acid or citric acid are preferred, but also esters of beta-hydroxypropionic acid, tartronic acid, D-gluconic acid, saccharic acid, mucic acid or glucuronic acid are suitable and particularly preferred are the esters of C ⁇ 2 - C ⁇ 5 fatty alcohols, for. B. are the commercial products Cosmacol ® from EniChem, Augusta Industriale,
  • Dicarboxylic acid esters such as di-n-butyl adipate, di- (2-ethylhexyl) adipate, di- (2-ethylhexyl) succinate and di-isotridecyiacelate as well as diol esters such as ethylene glycol dioleate, ethylene glycol di-isotridecanoate, propylene glycol di (2-ethylhexanoate), propylene glycol -di-isostearate, propylene glycol-di-pelargonate, butanediol-di-isostearate, neopentyl glycol dicaprylate, symmetrical, asymmetrical or cyclic esters of carbonic acid
  • Fatty alcohols e.g. B. glycerol carbonate or dicaprylyl carbonate (Cetiol ® CC), - Mono, - di- and trifatty acid esters of saturated and / or unsaturated linear and / or branched fatty acids with glycerin, e.g. B. Monomuls ® 90-O18, Monomuls ® 90-L12 or Cutina ® MD,
  • - Waxes in particular insect waxes such as beeswax and bumblebee wax, plant waxes such as candelilla wax and carnauba wax, fruit waxes, ozone kerit, micro waxes, ceresin, paraffin, triglycerides saturated and optionally hydroxylated Ci 6 - 3 o-fatty acids, such as.
  • Silicone compounds selected from decamethylcyclopentasiloxane, dodecamethylcyclohexasiloxane and silicone polymers, which can, if desired, be cross-linked, e.g. B. polydialkylsiloxanes, polyalkylarylsiloxanes, ethoxylated polydialkylsiloxanes, preferably the substances with the INCI name Dimethicone Copolyol, and polydialkylsiloxanes containing amine and / or hydroxy groups.
  • the amount of fatty substances used is 0.1 to 50% by weight, preferably 0.1 to 20% by weight and particularly preferably 0.1 to 15% by weight, in each case based on the total composition.
  • the skin treatment compositions according to the invention can furthermore contain one or more surface-active substances as an emulsifier or dispersant.
  • Emulsifiers cause water or oil-stable adsorption layers to form at the phase interface, which protect the dispersed droplets against coalescence and thus stabilize the emulsion.
  • emulsifiers are therefore made up of a hydrophobic and a hydrophilic part of the molecule. Hydrophilic emulsifiers preferably form O / W emulsions and hydrophobic emulsifiers preferably form W / O emulsions.
  • W / O emulsions which are stabilized without hydrophilic emulsifiers are disclosed in the published documents DE 19816665 A1 and DE 19801593 A1.
  • Under an emulsion is a droplet-like distribution (dispersion) of a liquid in another liquid with the use of energy to create stabilizing phase interfaces Understand surfactants.
  • the selection of these emulsifying surfactants or emulsifiers is based on the substances to be dispersed and the particular external phase as well as the fine particle size of the emulsion.
  • Emulsifiers which can be used according to the invention are, for example
  • alkyl (oligo) glucosides e.g. B. the commercially available product Montanov ® 68,
  • Sterols are understood to be a group of steroids which carry a hydroxyl group on the C atom 3 of the steroid structure and are isolated both from animal tissue (zoosterols) and from vegetable fats (phytosterols). Examples of zoosterols are cholesterol and lanosterol. Examples of suitable phytosterols are beta-sitosterol, stigmasterol, campesterol and ergosterol. Sterols, the so-called mycosterols, are also isolated from fungi and yeasts. - Phospholipids, especially the glucose phospholipids, which, for. B. as lecithins or phosphatidylcholines from z. B. egg yolk or plant seeds (e.g. soybeans) are obtained,
  • polyglycerols and polyglycerol preferably Polyglyceryl-2-dipolyhydroxy- stearate (commercial product Dehymuls ® PGPH) and polyglyceryl-3 diisostearate (Lameform ® TGI commercial product)
  • the cosmetic and pharmaceutical preparations according to the invention preferably contain the emulsifiers in amounts of 0.1 to 25% by weight, in particular 0.5-15% by weight, based on the total composition.
  • the skin treatment agents according to the invention can contain organic or mineral or modified mineral light protection filters.
  • the light protection filters are substances which are liquid or crystalline at room temperature and are able to absorb ultraviolet rays and absorb the energy in the form of longer-wave radiation, e.g. B. to release heat again.
  • the UVA and UVB filters can be used both individually and in mixtures. The use of filter mixtures is preferred according to the invention.
  • the organic UV filters used according to the invention are selected from the derivatives of dibenzoylmethane, cinnamic acid esters, diphenylacrylic acid esters, benzophenone, camphor, p-aminobenzoic acid esters, o-aminobenzoic acid esters, salicylic acid esters, benzimidazoles, 1, 3,5-triazines, monomeric and oligomeric 4,4- Diaryl butadiene carboxylic acid esters and carboxamides,
  • the organic UV filters can be oil-soluble or water-soluble. Oil-soluble UV filters which are particularly preferred according to the invention 1- (4-tert-butylphenyl) -3- (4'methoxyphenyl) propane-1, 3-dione (Parsol ® 1789), 1-phenyl-3- (4'-isopropylphenyl) -propane-1, 3- dione, 3- (4 ' -methylbenzylidene) -D, L-camphor, 4- (dimethylamino) -benzoic acid 2-ethylhexyl ester, 4- (dimethylamino) benzoic acid-2-octyl ester, 4- (dimethylamino) -benzoic acid amyl ester, 4- 2-ethylhexyl methoxycinnamate, propyl 4-methoxycinnamate, isopent
  • Preferred water-soluble UV filters are 2-phenylbenzimidazole-5-sulfonic acid and its alkali, alkaline earth, ammonium, alkylammonium, alkanolammonium and glucammonium salts, sulfonic acid derivatives of benzophenones, preferably 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid and their Salts, sulfonic acid derivatives of 3-benzylidene camphor, such as. B. 4- (2-oxo-3-bomylidenemethyl) benzenesulfonic acid and 2-methyl-5- (2-oxo-3-bornylidene) sulfonic acid and their salts.
  • the preferred inorganic light protection pigments according to the invention are finely dispersed metal oxides and metal salts, for example titanium dioxide, zinc oxide, iron oxide, aluminum oxide, cerium oxide, zirconium oxide, silicates (talc), barium sulfate and zinc stearate.
  • the particles should have an average diameter of less than 100 nm, preferably between 5 and 50 nm and in particular between 15 and 30 nm. They can have a spherical shape, but it is also possible to use particles which have an ellipsoidal shape or a shape which differs from the spherical shape in some other way.
  • the pigments can also be surface-treated, ie hydrophilized or hydrophobicized. Typical examples are coated titanium dioxide, such as. B.
  • Titanium dioxide T 805 (Degussa) or Eusolex ® T2000 (Merck). Silicones, and in particular trialkoxyoctylsilanes or simethicones, are particularly suitable as hydrophobic coating agents Question. So-called micro- or nanopigments are preferably used in sunscreens. Micronized zinc oxide is preferably used.
  • Contain protein hydrolyzates or their derivatives Contain protein hydrolyzates or their derivatives.
  • animal protein hydrolyzates are e.g. B. elastin, collagen, keratin, silk and milk protein protein hydrolyzates, which may also be in the form of salts.
  • Vegetable protein hydrolyzates e.g. B. soy, wheat, almond, pea, potato and rice protein hydrolyzates.
  • Corresponding commercial products are e.g. B. DiaMin ® (Diamalt), Gluadin ® (Cognis), Lexein ® (Inolex) and Crotein ® (Croda).
  • amino acid mixtures or individual amino acids such as arginine, lysine, histidine or pyrroglutamic acid, which have been obtained in some other way can also be used instead of them.
  • derivatives of protein hydrolyzates e.g. B. in the form of their fatty acid condensation products.
  • Corresponding commercial products are e.g. B. Lamepon ® (Cognis), Gluadin ® (Cognis), Lexein ® (Inolex), Crolastin ® or Crotein ® (Croda).
  • the cosmetic and pharmaceutical preparations according to the invention contain the additional protein hydrolyzates and their derivatives in amounts of 0.01-10% by weight, based on the total composition. Amounts of 0.1 to 5% by weight, in particular 0.1 to 3% by weight, are particularly preferred.
  • the skin treatment compositions according to the invention can furthermore contain mono-, oligo- or polysaccharides or their derivatives.
  • Suitable monosaccharides according to the invention are e.g. B. glucose, fructose, galactose, arabinose, ribose, xylose, lyxose, aliases, old rose, mannose, gulose, idose and talose, the deoxy sugar fucose and rhamnose and amino sugar such as z.
  • Glucose, fructose, galactose, arabinose and fucose are preferred; Glucose is particularly preferred.
  • Suitable oligosaccharides according to the invention are composed of two to ten monosaccharide units, for. B. sucrose, lactose or trehalose.
  • a particularly preferred oligosaccharide is sucrose.
  • honey which predominantly contains glucose and sucrose, is also particularly preferred.
  • Polysaccharides suitable according to the invention are composed of more than ten monosaccharide units.
  • Preferred polysaccharides are the starches made up of ⁇ -D-glucose units and starch degradation products such as amylose, amylopectin and dextrins.
  • Chemically and / or thermally modified starches eg. B. hydroxypropyl starch phosphate, dihydroxypropyl distarch phosphate or the commercial products Dry Flo ® .
  • Dextrans and their derivatives e.g. B. dextran sulfate.
  • nonionic cellulose derivatives such as methyl cellulose, hydroxypropyl cellulose or hydroxyethyl cellulose
  • cationic cellulose derivatives e.g. B. the commercial products Celquat ® and Polymer JR ® , and preferably Celquat ® H 100, Celquat ® L 200 and Polymer JR ® 400 (Polyquaternium-10) and Polyquaternium-24.
  • polysaccharides from fucose units e.g. B. the commercial product Fucogel ® .
  • the polysaccharides composed of amino sugar units, in particular chitins and their deacetylated derivatives, the chitosans and mucopolysaccharides, are particularly preferred.
  • the preferred mucopoly saccharides according to the invention include hyaluronic acid and its derivatives, e.g. B. sodium hyaluronate or dimethylsilanol hyaluronate, and chondroitin and its derivatives, e.g. B. chondroitin sulfate.
  • hyaluronic acid and its derivatives e.g. B. sodium hyaluronate or dimethylsilanol hyaluronate
  • chondroitin and its derivatives e.g. B. chondroitin sulfate.
  • the cosmetic and pharmaceutical preparations according to the invention can contain further plant extracts. They are usually obtained by extracting the entire plant, but in individual cases also exclusively from flowers and / or leaves and / or seeds and / or other parts of plants. posed. According to the invention, the extracts from the meristem, i.e.
  • Algae extracts can also be used to advantage.
  • the algae extracts used according to the invention come from green algae, brown algae, red algae or blue-green algae (cyanobacteria).
  • the algae used for the extraction can be of natural origin as well as obtained through biotechnological processes and, if desired, can be changed compared to the natural form.
  • the organisms can be changed genetically, by breeding or by cultivation in media enriched with selected nutrients.
  • Preferred algae extracts come from seaweed, blue-green algae, from the green algae Codium tomentosum and from the brown algae Fucus vesiculosus.
  • a particularly preferred algae extract comes from blue-green algae of the Spirulina species, which were cultivated in a magnesium-enriched medium.
  • the extracts from spirulina, green tea, aloe vera, meristem, witch hazel, apricot, marigold, guava, sweet potato, lime, mango, kiwi, cucumber, mallow, marshmallow and violet are particularly preferred.
  • the cosmetic and pharmaceutical preparations according to the invention can also contain mixtures of several, in particular two, different plant extracts.
  • the cosmetic and pharmaceutical preparations according to the invention can contain further active ingredients, auxiliaries and additives, for example:
  • Vitamins, provitamins and vitamin precursors from groups A, C, E and F in particular retinol (vitamin Ai) and its esters, e.g. the acetate and the
  • vitamin C ascorbic acid
  • palmitic acid esters glucosides
  • Phosphates of ascorbic acid, tocopherols, especially tocopherol and its esters e.g. B. the acetate, nicotinate, phosphate and succinate; also vitamin F, which is understood to mean essential fatty acids, in particular linoleic acid, linolenic acid and arachidonic acid;
  • Antioxidants for example amino acids (e.g. glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (e.g. urocanic acid) and their derivatives, peptides such as D, L-carnosine, D-carnosine, L- Carnosine and its derivatives (e.g. anserine), chlorogenic acid and its derivatives, lipoic acid and its derivatives (e.g. dihydroliponic acid), aurothioglucose, propylthiouracil and other thiols (e.g.
  • amino acids e.g. glycine, histidine, tyrosine, tryptophan
  • imidazoles e.g. urocanic acid
  • peptides such as D, L-carnosine, D-carnosine, L- Carnosine and its derivatives (e.g. anserine)
  • chlorogenic acid and its derivatives e.g.
  • thioredoxin glutathione, cysteine, cystine, cystamine and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl, ⁇ -linoleyl, cholesteryl and glyceryl esters) and their salts, dilauryl thiodipropionate, distearyl thiodipropionate , Thiodipropionic acid and its derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts) as well as sulfoximine compounds (e.g.
  • buthionine sulfoximines in very low tolerable doses (e.g. B. pmol to ⁇ mol / kg), further (Me tall) chelators (e.g. B. ⁇ -hydroxy fatty acids, palmitic acid, phytic acid, lactoferrin), humic acid, bile acid, bile extracts, bilirubin, biliverdin, EDTA, EGTA and their derivatives, unsaturated fatty acids and their derivatives (e.g.
  • ZnO, ZnSO 4 selenium and its derivatives (e.g. selenium methionine), stilbenes and their derivatives (e.g. stilbene oxide, trans-stilbene oxide) and the derivatives suitable as antioxidants (salts, esters, ethers, sugars, nucleotides, nucleosides, peptides and lipids) of these active ingredients,
  • Ceramides and pseudoceramides Triterpenes, especially triterpenic acids such as ursolic acid, rosmaric acid, betulinic acid, boswellic acid and bryonolic acid,
  • Monomeric catechins especially catechin and epicatechin, leucoanthocyanidins, catechin polymers (catechin tannins) and gallotannins,
  • - Thickeners e.g. B. gelatin, vegetable gums such as agar agar, guar gum, alginates, xanthan gum, gum arabic, karaya gum or locust bean gum, natural and synthetic clays and layered silicates, e.g. B. bentonite, hectorite, montmorillonite or Laponite ® , fully synthetic hydrocolloids such.
  • B. polyvinyl alcohol, and also Ca, Mg or Zn soaps of fatty acids,
  • Structurants such as maleic acid and lactic acid
  • Solvents, swelling and penetration substances such as ethanol, isopropanol, ethylene glycol, propylene glycol, propylene glycol monoethyl ether, glycerin and diethylene glycol, carbonates, hydrogen carbonates, guanidines, ureas and primary, secondary and tertiary phosphates
  • Opacifiers such as latex, styrene / PVP and styrene / acrylamide copolymers, pearlescent agents such as ethylene glycol mono- and distearate and PEG-3 distearate,
  • Blowing agents such as propane-butane mixtures, N 2 O, dimethyl ether, CO 2 and air.
  • the skin treatment agents according to the invention can contain one or more film-forming, emulsion-stabilizing, thickening or adhesive polymers, selected from natural and synthetic polymers, which can be cationic, anionic, amphoteric or non-ionic.
  • cationic polymers are polysiloxanes with quaternary groups, e.g. B. the commercial products Q2-7224 (Dow Corning), Dow Corning ® 929 emulsion (with Amodimethicone), SM-2059 (General Electric), SLM-55067 (Wacker) and Abil ® -Quat 3270 and 3272 (Th. Goldschmidt).
  • Preferred anionic polymers which can support the action of the active ingredient used according to the invention contain carboxylate and / or sulfonate groups and, for example, acrylic acid, methacrylic acid, crotonic acid, maleic anhydride and 2-acrylamido-2-methylpropanesulfonic acid as monomers.
  • the acidic groups can be present in whole or in part as sodium, potassium, ammonium, mono- or triethanolammonium salt.
  • Preferred monomers are 2-acrylamido-2-methylpropanesulfonic acid and acrylic acid.
  • anionic polymers contain 2-acrylamido-2-methylpropanesulfonic acid as the sole monomer or as comonomer, it being possible for the sulfonic acid group to be wholly or partly in salt form.
  • copolymers of at least one anionic monomer and at least one nonionic monomer are acrylamide, methacrylamide, acrylic acid ester, methacrylic acid ester, vinyl pyrrolidone, vinyl ether and vinyl ester.
  • Preferred anionic copolymers are acrylic acid-acrylamide copolymers and in particular polyacrylamide copolymers with monomers containing sulfonic acid groups.
  • a particularly preferred anionic copolymer consists of 70 to 55 mol% of acrylamide and 30 to 45 mol% of 2-acrylamido-2-methylpropanesulfonic acid, the sulfonic acid groups being wholly or partly as sodium, potassium, ammonium, mono- or triethanolammonium Salt.
  • This copolymer can also be crosslinked, the crosslinking agents preferably being polyolefinic Unsaturated compounds such as tetraallyloxyethane, allyl sucrose, allylpentaerythritol and methylene bisacrylamide are used.
  • Such a polymer is contained in the commercial product Sepigel ® 305 from SEPPIC.
  • the use of this compound has proven to be particularly advantageous in the context of the teaching according to the invention.
  • Polysorbate-80 sodium acryloyldimethyltaurate copoly- mers have proven effective as inventively particularly.
  • Other particularly preferred anionic homopolymers and copolymers are uncrosslinked and crosslinked polyacrylic acids. Allyl ethers of pentaerythritol, sucrose and propylene can be preferred crosslinking agents.
  • Such compounds are, for example, the commercial products Carbopol ® .
  • a particularly preferred anionic copolymer contains 80-98% of an unsaturated, optionally substituted C 3 as monomer. 6- carboxylic acid or its anhydride and, if desired, 2 to 20% substituted acrylic acid esters of saturated C 1 -C 30 -carboxylic acids, it being possible for the copolymer to be crosslinked with the aforementioned crosslinking agents.
  • Corresponding commercial products are Pemulen ® and the Carbopol ® types 954, 980, 1342 and ETD 2020 (ex BF Goodrich).
  • Suitable nonionic polymers are, for example, polyvinyl alcohols, which can be partially saponified, e.g. B. the commercial products Mowiol ® and vinyl pyrrolidone vinyl ester copolymers and polyvinyl pyrrolidones, which, for. B. are sold under the trademark Luviskol ® (BASF).
  • Further additives to the cosmetic or pharmaceutical skin treatment agents are selected from the vitamins, provitamins or vitamin precursors of the vitamin B group or their derivatives and the derivatives of 2-furanone.
  • the vitamin B group or the vitamin B complex include, among others
  • Vitamin Bi common name thiamine, chemical name 3 - [(4 ' -amino-2 ' - methyl-5 ' -pyrimidinyl) -methyl] -5- (2-hydroxyethyl) -4-methylthiazolium chloride.
  • Thiamine hydrochloride is preferably used in amounts of 0.05 to 1% by weight, based on the total agent.
  • Vitamin B 2 common name riboflavin, chemical name 7,8-dimethyl-10- (1-D-ribityl) -benzo [g] pteridine-2,4 (3 / - /, 10 / - /) - dione.
  • riboflavin comes e.g. B. in whey before, other riboflavin derivatives can be isolated from bacteria and yeast.
  • a stereoisomer of riboflavin which is also suitable according to the invention is lyxoflavin which can be isolated from fishmeal or liver and which carries a D-arabityl radical instead of D-ribityl.
  • Riboflavin or its derivatives are preferably used in amounts of 0.05 to 1% by weight, based on the total agent.
  • Vitamin B 3 • Vitamin B 3 .
  • the compounds nicotinic acid and nicotinamide (niacinamide) are often listed under this name.
  • the nicotinamide which is present in the cosmetic and pharmaceutical preparations according to the invention preferably in amounts of 0.05 to 1% by weight, based on the total composition, is preferred according to the invention.
  • Vitamin B 5 pantothenic acid and panthenol
  • Panthenol is preferably used.
  • Derivatives of panthenol which can be used according to the invention are, in particular, the esters and ethers of panthenol and cationically derivatized panthenols.
  • derivatives of 2-furanone with the general structural formula (I) can also be used.
  • the 2-furanone derivatives in which the substituents R 1 to R 6 independently of one another are a hydrogen atom, a hydroxyl radical, a methyl, methoxy, aminomethyl or hydroxymethyl radical, a saturated or mono- or di-unsaturated, linear or branched C 2 -C 4 - hydrocarbon radical, a saturated or mono- or di-unsaturated, represent branched or linear mono-, di- or trihydroxy-C 2 -C 4 - hydrocarbon residue or a saturated or mono- or di-unsaturated, branched or linear mono-, di- or triamino-C 2 -C 4 - hydrocarbon residue.
  • Particularly preferred derivatives are the commercially available substances dihydro-3-hydroxy-4,4-dimethyl-2 (3H) -furanone with the common name pantolactone (Merck), 4-hydroxymethyl- ⁇ -butyrolactone (Merck), 3.3 -Dimethyl-2-hydroxy- ⁇ -butyrolactone (Aldrich) and 2,5-dihydro-5-methoxy-2-furanone (Merck), all stereoisomers being expressly included.
  • the 2-furanone derivative which is extremely preferred according to the invention is pantolactone (dihydro-3-hydroxy-4,4-dimethyl-2 (3H) -furanone), wherein in formula (I) R 1 is a hydroxyl group, R 2 is a hydrogen atom , R 3 and R 4 represent a methyl group and R 5 and R 6 represent a hydrogen atom.
  • the stereoisomer (R) - pantolactone is formed when pantothenic acid is broken down.
  • the above-mentioned compounds of the vitamin B 5 type and the 2-furanone derivatives are preferably present in the cosmetic and pharmaceutical preparations according to the invention in a total amount of 0.05 to 10% by weight, based on the total composition. Total amounts of 0.1 to 5% by weight are particularly preferred.
  • Vitamin B ⁇ which does not mean a uniform substance, but rather the derivatives of 5-hydroxymethyl-2-methylpyhdin-3-ol known under the common names pyridoxine, pyridoxamine and pyridoxal.
  • Vitamin B 6 is contained in the cosmetic and pharmaceutical preparations according to the invention preferably in amounts of 0.0001 to 1.0% by weight, in particular in amounts of 0.001 to 0.01% by weight.
  • Vitamin B 7 also known as vitamin H or "skin vitamin”.
  • Biotin is (3aS, 4S, 6aR) -2-oxohexahydrothienol [3,4-] imidazole-4-valeric acid.
  • the cosmetic and pharmaceutical preparations according to the invention preferably contain biotin in amounts of 0.0001 to 1.0% by weight, in particular in amounts of 0.001 to 0.01% by weight.
  • Panthenol, pantolactone, nicotinamide and biotin are very particularly preferred according to the invention.
  • the cosmetic preparations used according to the invention are preferably suitable for the cosmetic treatment of cellulite and local excess fat, but also for use in so-called "slimming products" and for tightening the skin, in particular the skin of legs, décolleté, neck or in the facial area.
  • Another object of the invention is the use of a composition comprising a flavone, isoflavone or their glycoside and optionally a substance which stimulates and / or depolarizes C-nerve fibers for the production of a preparation for the therapeutic treatment of cellulite.
  • the active ingredients of the three groups mentioned above, optionally in combination with other active substances, together with one or more inert customary carriers and / or diluents for. B. with corn starch, milk sugar, cane sugar, sorbitol, microcrystalline cellulose, magnesium stearate, polyvinylpyrrolidone, citric acid, tartaric acid, water, water / ethanol, water / glycerol, water / sorbitol, water / polyethylene glycol, propylene glycol, carboxymethyl cellulose or fatty substances such as hard fat or the like suitable mixtures, work into conventional galenical preparations such as tablets, dragees, capsules, powders, suspensions, drops, ampoules, juices or suppositories.
  • the daily dosage of the active ingredient or mixture of active ingredients required to achieve a corresponding effect in pharmaceutical applications is advantageously 0.1 to 10 mg / kg body weight, preferably 0.5 to 2 mg / kg body weight.
  • compositions according to the invention are preferably suitable for the therapeutic treatment of cellulite.
  • the compositions according to the invention are prepared in that the aqueous phase, which contains water-soluble active ingredients and ingredients and, if appropriate, water-soluble emulsifiers, and the oil phase which contains fats, oils, oil-soluble active ingredients and optionally oil-soluble emulsifiers, at a temperature of 10 to 90 ° C are mixed intensively.
  • the anti-cellulite gel according to Example 1 with the formulation Gel-5 was tested for its effectiveness in relation to the cellulite phenomenon and its cosmetic acceptance in 25 women (half-side test against placebo).
  • the test participants were asked directly after the use test about the effectiveness of the product and the cosmetic acceptance in a standardized way.

Abstract

The invention relates to the use of a composition, comprising a flavone, an isoflavone or the glycoside thereof and optionally a material, which stimulates or depolarises C nerve fibres, in compositions for the cosmetic or pharmaceutical treatment of the cellulite.

Description

Verwendung von Flavonen oder Isoflavonen zur Cellulite-Behandlung Use of flavones or isoflavones for cellulite treatment
Die Erfindung betrifft die Verwendung einer Zusammensetzung, umfassend ein Flavon, Isoflavon oder ein Glykosid hiervon und gegebenenfalls einen Stoff der C- Nervenfasern stimuliert und/oder depolarisiert, zur kosmetischen oder pharmazeutischen Behandlung der Cellulite.The invention relates to the use of a composition comprising a flavone, isoflavone or a glycoside thereof and optionally a substance that stimulates and / or depolarizes the C-nerve fibers for the cosmetic or pharmaceutical treatment of cellulite.
Die Cellulite (Synonyme: Panniculosis, Lipodystrophie, Status protrusis cutis, Orangenhaut) ist eine lokale Ansammlung von Fett und Wasser in Körpergewebe. Sie stellt ein vorwiegend ästhetisches Problem dar, das mit Grübchenbildung und Vertiefungen der Haut und Knötchenbildung des subkutanen Fettgewebes insbesondere an Oberschenkeln und Gesäß einhergeht. Im Rahmen der vorliegenden Erfindung werden unter dem Begriff Cellulite auch lokale Fettübergewichte eingeschlossen. In fortgeschrittenen Stadien der Cellulite können auch Schmerzen im Bereich der Knötchen auftreten. Klar abzugrenzen von der Cellulite ist die Cellulitis (Panniculitis), die eine Entzündung des subkutanen Fettgewebes und damit eine in manchen Fällen schwere und lebensbedrohliche Erkrankung darstellt.Cellulite (synonyms: panniculosis, lipodystrophy, status protrusis cutis, orange peel) is a local accumulation of fat and water in body tissue. It is a predominantly aesthetic problem associated with pitting and deepening of the skin and nodulation of the subcutaneous fatty tissue, particularly on the thighs and buttocks. In the context of the present invention, local fat excess weights are also included under the term cellulite. In advanced stages of cellulite, pain in the area of the nodules can also occur. A clear distinction from cellulite is cellulitis (panniculitis), which is an inflammation of the subcutaneous adipose tissue and thus a serious and life-threatening illness in some cases.
Die Ursachen der Cellulite sind nicht genau bekannt. Sie wird aber in der Regel als kosmetisches Problem betrachtet. Es gibt jedoch auch Stimmen in der Fachliteratur, welche die Cellulite als einen krankhaften Zustand betrachten, der einer Therapie bedarf. Diese Betrachtungsweise gründet sich einerseits auf Schmerzzustände, welche besonders im Bereich der Lymphgefäße stark verfetteten subkutanen Gewebes ihren Ursprung haben. Andererseits kann sich die mit der Cellulite verbundene psychische Belastung in behandlungsbedürftigen psychosomatischen Störungen manifestieren.The causes of cellulite are not exactly known. However, it is usually considered a cosmetic problem. However, there are also voices in the specialist literature that regard cellulite as a pathological condition that requires therapy. This approach is based on the one hand on pain conditions, which have their origin especially in the area of the strongly greased subcutaneous tissue. On the other hand, those with cellulite manifest the associated psychological stress in psychosomatic disorders requiring treatment.
Die herkömmlichen Behandlungsmethoden der Cellulite versuchen, die Durchblutung zu fördern und die Bindegewebsstruktur positiv zu beeinflussen, beispielsweise durchThe conventional treatment methods for cellulite try to promote blood circulation and have a positive influence on the connective tissue structure, for example through
- Massage- massage
- Lymphdrainage- lymphatic drainage
- Diät und/oder Sport, wobei allerdings sogar eine Verschlechterung des Zustandes eintreten kann- Diet and / or exercise, although the condition may even worsen
- Magnetfelder- magnetic fields
- Liposuction (Fettabsaugung)- Liposuction (liposuction)
- Enzymtherapie, beispielsweise mit Hyaluronidase oder- Enzyme therapy, for example with hyaluronidase or
- Einnahme von Medikamenten zur Förderung der Lipolyse.- Taking medication to promote lipolysis.
Von den Verfahrensweisen einer Stimulation der Lipolyse ist diejenige am bekanntesten und am stärksten verbreitet, die darin besteht, das Enzym Phosphodiesterase zu inhibieren, um den Abbau des cyclischen AMP zu verhindern oder zumindest zu verlangsamen. Die Phosphodiesterase zerstört das cyclische AMP dadurch, dass sie es in 5'-AMP überführt, welches nicht mehr in der Lage ist, die Lipolyse zu aktivieren. Es ist also wichtig, die Wirkung der Phosphodiesterase in der Weise zu inhibieren, dass im Bereich der Adipocyten eine hohe Konzentration an cyclischem AMP erreicht wird mit dem Ziel, die Lipolyse zu stimulieren. Unter den verschiedenen Phosphodiesterase-Inhibitoren, die beispielsweise als Abmagerungsmittel empfohlen wurden, sind die Xanthin-Basen, insbesondere Coffein, zu nennen.The best known and most widespread of the methods of stimulating lipolysis is to inhibit the enzyme phosphodiesterase in order to prevent or at least slow down the degradation of the cyclic AMP. The phosphodiesterase destroys the cyclic AMP by converting it to 5 ' -AMP, which is no longer able to activate lipolysis. It is therefore important to inhibit the action of the phosphodiesterase in such a way that a high concentration of cyclic AMP is achieved in the region of the adipocytes with the aim of stimulating lipolysis. Among the various phosphodiesterase inhibitors that have been recommended, for example, as slimming agents, are the xanthine bases, especially caffeine.
Weiterhin wurden unter anderem Pflanzenextrakte, Wachstumsfaktoren, Inositolphosphat, Alpha-Hydroxycarbonsäuren und Vitamin C zur Behandlung der Cellulite empfohlen. Die FR 2740681 beschreibt kosmetische Zusammensetzungen zur Behandlung der Cellulite, welche Coffein und einen Extrakt aus der Rinde oder den Blättern von Pflanzen der Gattung Viburnum enthalten. Als ein Bestandteil dieses Extrakts ist Amentoflavon beschrieben, ein aus zwei Apigenin-Einheiten bestehendes Biflavonoid. Amentoflavon stellt nach der Lehre dieser Schrift einen charakteristischen Inhaltsstoff von Viburnum dar und dient zur Standardisierung der Dosierung des Viburnum-Extrakts in den erfindungsgemäßen Zusammensetzungen. Die Schrift gibt dem Fachmann keinen Hinweis darauf, dass das Amentoflavon für die Anti-Cellulite-Wirkung der Zusammensetzungen ursächlich oder mitverantwortlich sein könnte.Plant extracts, growth factors, inositol phosphate, alpha-hydroxycarboxylic acids and vitamin C were also recommended for the treatment of cellulite. FR 2740681 describes cosmetic compositions for the treatment of cellulite which contain caffeine and an extract from the bark or leaves of plants of the genus Viburnum. Amentoflavon, a biflavonoid consisting of two apigenin units, is described as a component of this extract. According to the teaching of this document, amentoflavone is a characteristic ingredient of viburnum and serves to standardize the dosage of the viburnum extract in the compositions according to the invention. The document does not give the person skilled in the art any indication that the amentoflavone could be the cause or jointly responsible for the anti-cellulite effect of the compositions.
Die FR 2609395 beschreibt Xanthin-haltige pharmazeutische oder kosmetische Zusammensetzungen mit einem lokalen schlankmachenden Effekt, der auf ihre intrazelluläre Phosphodiesterase-inhibierende Wirkung zurückgeführt wird. Die Zusammensetzungen können als zusätzliche Bestandteile Glykoside wie beispielsweise Bioflavonoide enthalten. Welche Stoffe oder Stoffgruppen unter dem in der Fachwelt bekanntermaßen widersprüchlich ausgelegten Begriff Bioflavonoide zu verstehen sind, wird nicht offenbart. Der Fachmann wird dadurch nicht in die Lage versetzt, eine der Lehre der Schrift entsprechende Zusammensetzung mit einem Gehalt an einem Bioflavonoid zuzubereiten, welche einen lokal schlankmachenden Effekt ausübt. Die Schrift gibt auch keinerlei Hinweise darauf, dass die Bioflavonoide zu den schlankmachenden Eigenschaften der erfindungsgemäßen Zusammensetzungen beitragen könnten.FR 2609395 describes xanthine-containing pharmaceutical or cosmetic compositions with a local slimming effect which is attributed to their intracellular phosphodiesterase-inhibiting action. The compositions may contain glycosides such as bioflavonoids as additional ingredients. It is not disclosed which substances or groups of substances are to be understood under the term bioflavonoids, which is known to be contradictory in the specialist world. This does not enable the person skilled in the art to prepare a composition according to the teaching of the writing containing a bioflavonoid which has a locally slimming effect. The document also gives no indication that the bioflavonoids could contribute to the slimming properties of the compositions according to the invention.
Aus der JP 08099813 sind aus Pflanzenmaterial gewonnene Stoffe bekannt, die neben anderen Stoffen Capsaicin, Flavonoide und/oder Isoflavone enthalten können. Die dort beschriebenen Stoffe dienen zur Regulation des Pflanzenwachstums in der Landwirtschaft, sonstige Anwendungen sind nicht erwähnt.From JP 08099813 substances obtained from plant material are known which, in addition to other substances, can contain capsaicin, flavonoids and / or isoflavones. The substances described there serve to regulate plant growth in agriculture, other applications are not mentioned.
Aus der JP 11060460 sind Capsaicin und Vanillyl-nonylamid als Bestandteile hautkosmetischer Zubereitungen bekannt, welche ein durch exotherm reagierende Substanzen erzeugtes Wärmegefühl auf der Haut verstärken. Die Schrift gibt jedoch keine Hinweise darauf, dass sich diese Zubereitungen zur Behandlung der Cellulite eignen könnten.From JP 11060460 capsaicin and vanillyl nonylamide are known as constituents of skin cosmetic preparations which intensify a feeling of warmth on the skin produced by exothermic substances. However, the scripture gives no evidence that these preparations could be used to treat cellulite.
Die aus dem Stand der Technik bekannten Stoffe und Verfahren zur Behandlung der Cellulite sind nicht befriedigend, insbesondere was das Ausmaß und die Geschwindigkeit des Behandlungseffektes angeht.The substances and methods for treating cellulite known from the prior art are unsatisfactory, particularly as regards the extent and speed of the treatment effect.
Aufgabe der Erfindung war es, den Mängeln des Stands der Technik abzuhelfen und verbesserte Mittel zur Behandlung der Cellulite bereitzustellen.The object of the invention was to remedy the shortcomings of the prior art and to provide improved agents for treating cellulite.
Die erfindungsgemäße Aufgabe wird gelöst durch die Verwendung einer Zusammensetzung, umfassend ein Flavon, Isoflavon oder deren Glykosid und gegebenenfalls einen Stoff, welcher C-Nervenfasern stimuliert und/oder depolarisiert, zur kosmetischen Behandlung von Cellulite oder zur Straffung der Haut.The object of the invention is achieved by the use of a composition comprising a flavone, isoflavone or their glycoside and optionally a substance which stimulates and / or depolarizes carbon nerve fibers, for the cosmetic treatment of cellulite or for firming the skin.
Gegenstand der Erfindung ist demnach weiterhin die Verwendung einer Zusammensetzung, umfassend ein Flavon, Isoflavon oder deren Glykosid und gegebenenfalls einen Stoff, der C-Nervenfasern stimuliert und/oder depolarisiert, zur Herstellung einer pharmazeutischen Zubereitung zur therapeutischen Behandlung von Cellulite.The invention accordingly furthermore relates to the use of a composition comprising a flavone, isoflavone or their glycoside and, if appropriate, a substance which stimulates and / or depolarizes C-nerve fibers, for the production of a pharmaceutical preparation for the therapeutic treatment of cellulite.
Unter Flavonen sind im Sinne der vorliegenden Erfindung Stoffe zu verstehen, die Hydrierungs-, Oxidations- oder Substitutionsprodukte des 2-Phenyl-4H-1- benzopyrans darstellen, wobei eine Hydrierung in der 2,3-Stellung des Kohlenstoffgerüsts vorliegen kann, eine Oxidation unter Ausbildung einer Carbonylgruppe in der 4-Stellung vorliegen kann, und unter Substitution der Ersatz eines oder mehrerer Wasserstoffatome durch Hydroxy- oder Methoxy-Gruppen zu verstehen ist. Bei dieser Definition sind also Flavane, Flavan-3-ole (Catechine), Flavan-3,4-diole (Leukoanthocyanidine), Flavone, Flavonole und Flavanone im herkömmlichen Sinn eingeschlossen. Zu den erfindungsgemäßen Flavonen zählen beispielsweise Chrysin, Galangin, Apigenin, Fisetin, Luteolin, Kampferöl, Quercetin, Mo n, Robinetin, Gossypetin, Taxifolin, Myricetin, Rhamnetin, Isorhamnetin, Naringenin, Eriodyctiol, Hesperetin, Liquiritigenin, Catechin und Epicatechin. Als Flavone bevorzugt sind Quercetin und Luteolin.For the purposes of the present invention, flavones are understood to mean substances which are hydrogenation, oxidation or substitution products of 2-phenyl-4H-1-benzopyran, where hydrogenation can be present in the 2,3-position of the carbon skeleton, oxidation under Formation of a carbonyl group may be in the 4-position, and substitution is to be understood as the replacement of one or more hydrogen atoms by hydroxyl or methoxy groups. This definition therefore includes flavans, flavan-3-oles (catechins), flavan-3,4-diols (leucoanthocyanidins), flavones, flavonols and flavanones in the conventional sense. The flavones according to the invention include, for example, chrysin, galangin, apigenin, fisetin, luteolin, camphor oil, quercetin, Mon, Robinetin, Gossypetin, Taxifolin, Myricetin, Rhamnetin, Isorhamnetin, Naringenin, Eriodyctiol, Hesperetin, Liquiritigenin, Catechin and Epicatechin. Quercetin and luteolin are preferred as flavones.
In den erfindungsgemäßen Flavon-Giykosiden sind die Flavone über mindestens eine Hydroxygruppe mit mindestens einem Zucker glykosidisch verknüpft. Als Zucker kommen Mono- und Oligosaccharide, insbesondere D-Glucose, D-Galactose, D- Glucuronsäure, D-Galacturonsäure, D-Xylose, D-Apiose, L-Rhamnose, L-Arabinose und Rutinose in Betracht. Beispiele für die erfindungsgemäßen Flavon-Glykoside sind Rutin, Hesperidin und Naringin.In the flavone glycosides according to the invention, the flavones are glycosidically linked to at least one sugar via at least one hydroxyl group. Monosaccharides and oligosaccharides, in particular D-glucose, D-galactose, D-glucuronic acid, D-galacturonic acid, D-xylose, D-apiose, L-rhamnose, L-arabinose and rutinose are suitable as sugars. Examples of the flavone glycosides according to the invention are rutin, hesperidin and naringin.
Unter Isoflavonen sind im Sinne der vorliegenden Erfindung Stoffe zu verstehen, die Hydrierungs-, Oxidations- oder Substitutionsprodukte des 3-Phenyl-4H-1- benzopyrans darstellen, wobei eine Hydrierung in der 2,3-Stellung des Kohlenstoffgerüsts vorliegen kann, eine Oxidation unter Ausbildung einer Carbonylgruppe in der 4-Stellung vorliegen kann, und unter Substitution der Ersatz eines oder mehrerer Wasserstoffatome durch Hydroxy- oder Methoxy-Gruppen zu verstehen ist. Zu den erfindungsgemäßen Isoflavonen zählen beispielsweise Daidzein, Genistein, Prunetin, Biochanin, Orobol, Santal, Pratensein, Irigenin, Glycitein, Biochanin A und Formononetin. Als Isoflavone bevorzugt sind Daidzein, Genistein, Glycitein und Formononetin.For the purposes of the present invention, isoflavones are understood to mean substances which are hydrogenation, oxidation or substitution products of 3-phenyl-4H-1-benzopyran, where hydrogenation can be present in the 2,3-position of the carbon skeleton, oxidation under Formation of a carbonyl group may be in the 4-position, and substitution is to be understood as the replacement of one or more hydrogen atoms by hydroxyl or methoxy groups. The isoflavones according to the invention include, for example, daidzein, genistein, prunetin, biochanin, Orobol, Santal, pratensein, irigenin, glycitein, biochanin A and formononetin. Daidzein, genistein, glycitein and formononetin are preferred as isoflavones.
In den erfindungsgemäßen Isoflavon-Glykosiden sind die Isoflavone über mindestens eine Hydroxygruppe mit mindestens einem Zucker glykosidisch verknüpft. Als Zucker kommen Mono- oder Oligosaccharide, insbesondere D- Glucose, D-Galactose, D-Glucuronsäure, D-Galacturonsäure, D-Xylose, D-Apiose, L- Rhamnose, L-Arabinose und Rutinose in Betracht. Bevorzugte Beispiele für die erfindungsgemäßen Isoflavon-Glykoside sind Daidzin und Genistin.In the isoflavone glycosides according to the invention, the isoflavones are glycosidically linked to at least one sugar via at least one hydroxyl group. Suitable sugars are mono- or oligosaccharides, in particular D-glucose, D-galactose, D-glucuronic acid, D-galacturonic acid, D-xylose, D-apiose, L-rhamnose, L-arabinose and rutinose. Preferred examples of the isoflavone glycosides according to the invention are daidzin and genistin.
Die C-Nervenfasern, auch polymodale C-Nervenfasern genannt, spielen im menschlichen Organismus eine wichtige Rolle für die sensorischen Funktionen des Körpers, insbesondere der Haut. Sie sind vor allem an der Wahrnehmung beispielsweise von Wärme, Kälte und Juckreiz sowie dem Schmerzempfinden (z. B. Hitzeschmerz, Kälteschmerz, Stechschmerz, Brennschmerz) beteiligt. Eine Sonderstellung nehmen die polymodalen C-Nervenfasern als Untergruppe der C- Nervenfasern ein, da sie auf mehrere unterschiedliche Reize reagieren können und darüber hinaus durch die Freisetzung von Mediatoren ihrerseits in das Reizgeschehen eingreifen können. An der Oberfläche der C-Nervenfasern befinden sich unterschiedliche Rezeptoren wie beispielsweise Capsaicin-, Bradykinin- und 5- Hydroxytryptamin-Rezeptoren, sowie lonenkanäle wie beispielsweise Calcium- und Natrium-Kanäle, über welche die C-Nervenfasern stimuliert und/oder depolarisiert werden können. Über diese Stimulation und/oder Depolahsation wird ein sensorischer Reiz ausgelöst, der sich beispielsweise als Brennen, Prickeln, Wärme-, Kälte- oder Schmerzempfinden bemerkbar macht. Im Sinne der vorliegenden Erfindung ist es bevorzugt, durch die Stimulation und/oder Depolahsation der C- Nervenfasern der Haut, insbesondere durch eine Stimulation der Capsaicin- Rezeptoren dieser Nervenfasern, ein Prickeln, leichtes Brennen oder ein Wärmeoder Kältegefühl auszulösen.The C-nerve fibers, also called polymodal C-nerve fibers, play an important role in the human organism for the sensory functions of the body, especially the skin. They are primarily perception for example from warmth, cold and itching as well as the sensation of pain (e.g. heat pain, cold pain, stinging pain, burning pain). The polymodal C-nerve fibers have a special position as a sub-group of the C-nerve fibers because they can react to several different stimuli and can also intervene in the stimulus process through the release of mediators. Different receptors such as capsaicin, bradykinin and 5-hydroxytryptamine receptors are located on the surface of the C-nerve fibers, as well as ion channels such as calcium and sodium channels, via which the C-nerve fibers can be stimulated and / or depolarized. This stimulation and / or depolarization triggers a sensory stimulus which manifests itself, for example, as a burning sensation, tingling sensation, warmth, coldness or pain. For the purposes of the present invention, it is preferred to trigger a tingling sensation, a slight burning sensation or a feeling of warmth or coldness by stimulating and / or depolarizing the C-nerve fibers of the skin, in particular by stimulating the capsaicin receptors of these nerve fibers.
Unter C-Nervenfasern beeinflussenden Stoffen sind im Rahmen der vorliegenden Erfindung beispielsweise zu verstehen:In the context of the present invention, substances influencing C nerve fibers are to be understood, for example:
- Capsaicin- capsaicin
- Extrakte von rotem Pfeffer oder Cayennepfeffer- Red pepper or cayenne pepper extracts
- Vanillyl-nonylamid (Nonivamide)- Vanillyl nonylamide (nonivamide)
- Säureamide des 4-Hydroxy-3-methoxy-benzylamins mit Carbonsäuren R-COOH, wobei die Carbonsäuren ausgewählt sind aus der Gruppe gebildet von geradkettigen oder verzweigten Alkylcarbonsäuren mit 1 bis 22 Kohlenstoffatomen- Acid amides of 4-hydroxy-3-methoxy-benzylamine with carboxylic acids R-COOH, the carboxylic acids being selected from the group consisting of straight-chain or branched alkyl carboxylic acids having 1 to 22 carbon atoms
- Extrakte von Ingwer- Ginger extracts
- die über die vorstehend aufgeführten Stoffe hinaus in der JP 11060460 beschriebenen, ein Wärmegefühl bewirkenden Stoffe sowie Glykoside der vorstehend genannten Stoffe, soweit diese zur Bildung von Glykosiden befähigt sind. In diesen Glykosiden sind die vorstehend genannten Stoffe, soweit sie eine oder mehrere Hydroxygruppen enthalten, über mindestens eine Hydroxygruppe mit einem Zucker glykosidisch verknüpft. Als Zucker kommen insbesondere D-Glucose, D-Galactose, D-Glucuronsäure, D-Galacturonsäure, D- Xylose, D-Apiose, L-Rhamnose, L-Arabinose und D-Maltose in Betracht. Weitere geeignete Stoffe sind beschrieben in P. D. Wall und R. Melzack (Eds.), Textbook of Pain, Churchill Livingstone Verlag, Edinburgh 1994, S. 13 bis 37 und 58 bis 72.- In addition to the substances listed above in JP 11060460, heat-causing substances and glycosides of the aforementioned substances, insofar as they are capable of forming glycosides. In these glycosides, the substances mentioned above, insofar as they contain one or more hydroxyl groups, are at least a hydroxy group is glycosidically linked to a sugar. Particularly suitable sugars are D-glucose, D-galactose, D-glucuronic acid, D-galacturonic acid, D-xylose, D-apiose, L-rhamnose, L-arabinose and D-maltose. Other suitable substances are described in PD Wall and R. Melzack (Eds.), Textbook of Pain, Churchill Livingstone Verlag, Edinburgh 1994, pp. 13 to 37 and 58 to 72.
Als C-Nervenfasern beeinflussende Stoffe bevorzugt sind Capsaicin, N-Vanillyl- nonanamid sowie deren Glykoside.Preferred substances influencing C-nerve fibers are capsaicin, N-vanillyl nonanamide and their glycosides.
Ein Vorteil der erfindungsgemäßen Zubereitungen mit Stoffen, die C-Nervenfasern stimulieren und/oder depolarisieren, ist die Erzeugung eines, vom Behandlungseffekts auf die Cellulite unabhängigen, physiologischen und/oder psychologischen Effekts, der dem Anwender bereits unmittelbar während oder nach der Anwendung des Mittels den subjektiven Eindruck eines Wirkungseintritts vermittelt. Die Verbesserung der Cellulite durch die erfindungsgemäßen Zubereitungen kommt insbesondere durch den Abbau von Fettzellen und den Umbau von Bindegewebe zustande, weshalb der Behandlungserfolg physiologisch bedingt erst nach längerer Anwendung sichtbar wird. In der Praxis hat sich aber gezeigt, dass die Benutzer eines Anti-Cellulite-Mittels die Anwendung des Mittels sehr bald wieder einstellen und von dem verwendeten Produkt enttäuscht sind, wenn sie nicht zumindest den subjektiven Eindruck haben, dass das Mittel eine Wirkung ausübt. In den erfindungsgemäßen Zubereitungen löst die Anwesenheit von Stoffen, die C-Nervenfasern stimulieren und/oder depolarisieren, beim Anwender einen sensorisch wahrnehmbaren Reiz aus, welcher ihm subjektiv einen Wirkungseindruck vermittelt.An advantage of the preparations according to the invention with substances that stimulate and / or depolarize C-nerve fibers is the generation of a physiological and / or psychological effect which is independent of the treatment effect on cellulite and which the user already has immediately during or after the application of the agent gives a subjective impression of an onset of effect. The improvement in cellulite by the preparations according to the invention is achieved in particular by the breakdown of fat cells and the remodeling of connective tissue, which is why the success of the treatment becomes visible only after prolonged use due to physiological reasons. In practice, however, it has been shown that the users of an anti-cellulite agent very soon stop using the agent and are disappointed with the product used if they do not at least have the subjective impression that the agent has an effect. In the preparations according to the invention, the presence of substances which stimulate and / or depolarize C-nerve fibers triggers a sensible stimulus in the user, which subjectively gives him an impression of the effect.
Darüber hinaus haben die C-Nervenfasern beeinflussenden Stoffe teilweise noch weitere erwünschte Wirkungen. So fördern sie die Durchblutung des behandelten Gewebes und begünstigen damit die Penetration der Inhaltsstoffe der Zubereitung in die Haut. Weiter kann dadurch der Abtransport der Abbauprodukte gefördert werden, welche im Verlauf der Lipolyse entstehen, die durch die Anwendung der Zubereitung bewirkt wird. Darüber hinaus kann der in schweren Fällen auftretende Cellulite- Schmerz gedämpft werden. Dies ist beispielsweise der Fall, wenn Nonivamid (N- Vanillyl-nonanamid) als die C-Nervenfasern beeinflussende Substanz verwendet wird.In addition, the substances that influence the C-nerve fibers sometimes have other desired effects. They promote the blood flow to the treated tissue and thus promote the penetration of the ingredients of the preparation into the skin. Furthermore, the removal of the degradation products which arise in the course of the lipolysis which is brought about by the use of the preparation can be promoted. In addition, cellulite in severe cases Pain be dampened. This is the case, for example, when nonivamide (N-vanillyl-nonanamide) is used as the substance influencing the C-nerve fibers.
Die Wirkstoffe werden erfindungsgemäß in solchen Konzentrationen verwendet, dass die toxikologisch zulässigen Einsatzkonzentration in Zubereitungen bzw. bei der Anwendung nicht überschritten werden.The active substances are used according to the invention in concentrations such that the toxicologically permissible use concentration in preparations or during use is not exceeded.
Erfindungsgemäß weiterhin bevorzugt ist es, wenn die Flavone, Isoflavone und deren Glykoside als Bestandteile eines aus einer Pflanze gewonnenen Substanzgemisches, insbesondere eines pflanzlichen Extraktes, in den Zubereitungen enthalten sind. Solche pflanzlichen Substanzgemische können in dem Fachmann geläufiger Weise beispielsweise durch Auspressen oder Extrahieren aus Pflanzen wie Soja, Rotklee oder Kichererbsen gewonnen werden. Besonders bevorzugt werden in den erfindungsgemäßen Zubereitungen Isoflavone oder Isoflavon-Glykoside in Form von aus Soja gewonnenen Extrakten eingesetzt, wie sie beispielsweise unter der Produktbezeichnung Soy Protein Isolate SPI (Protein Technology International, St. Louis) oder Soy Phytochemicals Concentrate SPC (Archer Daniels Midland, Decatur) im Handel erhältlich sind.It is further preferred according to the invention if the preparations contain the flavones, isoflavones and their glycosides as constituents of a mixture of substances obtained from a plant, in particular a plant extract. Such vegetable substance mixtures can be obtained in a manner familiar to the person skilled in the art, for example by pressing or extracting them from plants such as soybean, red clover or chickpeas. Isoflavones or isoflavone glycosides in the form of extracts obtained from soy are particularly preferably used in the preparations according to the invention, such as those known under the product name Soy Protein Isolate SPI (Protein Technology International, St. Louis) or Soy Phytochemicals Concentrate SPC (Archer Daniels Midland, Decatur) are commercially available.
Als Extraktionsmittel zur Herstellung der genannten Pflanzenextrakte können u. a.As an extractant for the production of the plant extracts mentioned, u. a.
Wasser, Alkohole sowie deren Mischungen verwendet werden. Unter den Alkoholen sind dabei niedere Alkohole wie vor allem Ethanol und Isopropanol, und mehrwertigeWater, alcohols and mixtures thereof can be used. Among the alcohols are lower alcohols such as especially ethanol and isopropanol, and polyvalent ones
Alkohole wie Ethylenglykol, Propylenglykol und Butylenglykol und zwar sowohl als alleiniges Extraktionsmittel als auch in Mischung mit Wasser, bevorzugt. DieAlcohols such as ethylene glycol, propylene glycol and butylene glycol, both as the sole extracting agent and in a mixture with water, are preferred. The
Wasserdampfdestillation fällt erfindungsgemäß unter die bevorzugtenSteam distillation is one of the preferred in the present invention
Extraktionsverfahren.Extraction process.
Erfindungsgemäß bevorzugt ist die alkoholische Extraktion.Alcoholic extraction is preferred according to the invention.
Weiterhin kann es bevorzugt sein, in den erfindungsgemäßen Mitteln Mischungen aus mehreren, insbesondere aus zwei, verschiedenen Pflanzenextrakten einzusetzen. In einer weiteren Ausführungsform betrifft die Erfindung die Verwendung einer Zusammensetzung, umfassend ein Flavon, Isoflavon oder deren Glykosid und gegebenenfalls einen Stoff, der C-Nervenfasern stimuliert und/oder depolarisiert, in Kombination mit einem Phosphodiesterase-Inhibitor zur kosmetischen Behandlung von Cellulite oder zur Herstellung einer pharmazeutischen Zubereitung zur therapeutischen Behandlung von Cellulite.Furthermore, it may be preferred to use mixtures of several, in particular two, different plant extracts in the agents according to the invention. In a further embodiment, the invention relates to the use of a composition comprising a flavone, isoflavone or their glycoside and, if appropriate, a substance which stimulates and / or depolarizes C-nerve fibers, in combination with a phosphodiesterase inhibitor for the cosmetic treatment of cellulite or for the preparation a pharmaceutical preparation for the therapeutic treatment of cellulite.
Als Phosphodiesterase-inhibitoren kommen dabei erfindungsgemäß beispielsweise Inhibitoren in Betracht, wie sie beschrieben sind in R. M. Di Salvo, Controlling the Appearance of Cellulite, Cosmetics and Toiletries Magazine 110, S. 50-59 (1995) oder in L. Stryer, Biochemie, Spektrum Akademischer Verlag GmbH, Heidelberg 1991 , S. 482.According to the invention, suitable phosphodiesterase inhibitors are, for example, inhibitors as described in RM Di Salvo, Controlling the Appearance of Cellulite, Cosmetics and Toiletries Magazine 110, pp. 50-59 (1995) or in L. Stryer, Biochemie, Spektrum Akademischer Verlag GmbH, Heidelberg 1991, p. 482.
Als Phosphodiesterase-inhibitoren kommen erfindungsgemäß bevorzugt Xanthin oder ein Methylxanthin in Betracht, wobei unter Methylxanthin ein Xanthin-Derivat zu verstehen ist, in dem ein oder mehrere Wasserstoffatome durch Methylgruppen ersetzt sind. Als Methylxanthine bevorzugt sind Theophyllin, Theobromin und Coffein, besonders bevorzugt ist Coffein.According to the invention, xanthine or a methylxanthine are preferably considered as phosphodiesterase inhibitors, methyl xanthine being a xanthine derivative in which one or more hydrogen atoms are replaced by methyl groups. Theophylline, theobromine and caffeine are preferred as methylxanthines, and caffeine is particularly preferred.
Gemäß der Erfindung enthalten die kosmetischen oder pharmazeutischen Zubereitungen insgesamt 0,1 bis 20 Gew.-%, und vorzugsweise 1 bis 10 Gew.-% eines oder mehrerer Flavone, Isoflavone oder deren Glykosiden sowie gegebenenfalls 0,0001 bis 3 Gew.-% und vorzugsweise 0,005 bis 0,5 Gew.-% an einem oder mehreren, die C-Nervenfasern stimulierenden und/oder depolarisierenden Stoffen bezogen auf das Gesamtgewicht der Zubereitung.According to the invention, the cosmetic or pharmaceutical preparations contain a total of 0.1 to 20% by weight, and preferably 1 to 10% by weight, of one or more flavones, isoflavones or their glycosides and optionally 0.0001 to 3% by weight and preferably 0.005 to 0.5% by weight of one or more substances which stimulate and / or depolarize the C nerve fibers, based on the total weight of the preparation.
In einer weiteren Ausführungsform der Erfindung enthalten die kosmetischen oder pharmazeutischen Zubereitungen zusätzlich insgesamt 1 bis 15 Gew.-%, und vorzugsweise 5 bis 10 Gew.-% eines oder mehrerer Phosphodiesterase-inhibitoren, bezogen auf das Gesamtgewicht der Zubereitung. Es wurde insbesondere überraschend festgestellt, dass die erfindungsgemäße Kombination ausIn a further embodiment of the invention, the cosmetic or pharmaceutical preparations additionally contain a total of 1 to 15% by weight, and preferably 5 to 10% by weight, of one or more phosphodiesterase inhibitors, based on the total weight of the preparation. In particular, it was surprisingly found that the combination according to the invention consists of
(a) einem oder mehreren Flavonen, Isoflavonen oder deren Glykosiden(a) one or more flavones, isoflavones or their glycosides
(b) einem oder mehreren die C-Nervenfasern stimulierenden und/oder depolarisierenden Stoffen(b) one or more substances that stimulate and / or depolarize the C-nerve fibers
(c) einem oder mehreren Phosphodiesterase-inhibitoren eine unerwartet hohe Wirkung bei der Behandlung der Cellulite zeigen, wie sie nur durch einen synergistischen Effekt der Komponenten erklärt werden kann.(c) show one or more phosphodiesterase inhibitors an unexpectedly high effect in the treatment of cellulite, as can only be explained by a synergistic effect of the components.
In einer weiteren Ausführungsform der Erfindung enthalten die kosmetischen oder pharmazeutischen ZubereitungenIn a further embodiment of the invention, the cosmetic or pharmaceutical preparations contain
(a) 0,1 bis 20, und vorzugsweise 1 bis 10 Gew.-% an einem oder mehreren Flavonen, Isoflavonen oder deren Glykosiden(a) 0.1 to 20, and preferably 1 to 10 wt .-% of one or more flavones, isoflavones or their glycosides
(b) 0,0001 bis 3, und vorzugsweise 0,005 bis 0,5 Gew.-% an einem oder mehreren die C-Nervenfasern stimulierenden und/oder depolarisierenden Stoffen(b) 0.0001 to 3, and preferably 0.005 to 0.5% by weight of one or more substances which stimulate and / or depolarize the C-nerve fibers
(c) 1 bis 15, und vorzugsweise 5 bis 10 Gew.-% an einem oder mehreren Phosphodiesterase-inhibitoren jeweils bezogen auf das Gesamtgewicht der Zubereitung.(c) 1 to 15, and preferably 5 to 10% by weight of one or more phosphodiesterase inhibitors, in each case based on the total weight of the preparation.
Die erfindungsgemäße kosmetische Verwendung der Zusammensetzung, umfassend ein Flavon, Isoflavon oder deren Glykosid und gegebenenfalls einen Stoff, der C-Nervenfasern stimuliert und/oder depolarisiert, erfolgt bevorzugt zusammen mit einem physiologisch verträglichen Träger in Form einer kosmetischen Zubereitung.The cosmetic use according to the invention of the composition, comprising a flavone, isoflavone or their glycoside and optionally a substance which stimulates and / or depolarizes C-nerve fibers, is preferably carried out together with a physiologically tolerable carrier in the form of a cosmetic preparation.
Der physiologisch verträgliche Träger der kosmetischen oder pharmazeutischen Zubereitungen umfaßt ein oder mehrere Adjuvantien, wie sie üblicherweise in solchen Zubereitungen verwendet werden, wie z. B. Fette, Öle, Wachse, Silikone, Emulgatoren, Alkohole, Polyole, Verdickungsmittel, anfeuchtende und/oder feuchthaltende Substanzen, Tenside, Weichmacher, Schaumbremsen, anionische, kationische, nichtionische oder amphotere Polymere, Alkalinisierungs- oder Acidifizierungsmittel, Enthärter, Adsorbentien, Lichtschutzmittel, Elektrolyte, Sequestrierungsmittel, organische Lösungsmittel, Konservierungsmittel, Bakterizide, Antioxidantien, Vitamine, Duftstoffe, Aromen, Süßungsmittel, Farbstoffe und Pigmente.The physiologically acceptable carrier of the cosmetic or pharmaceutical preparations comprises one or more adjuvants, as are usually used in such preparations, such as. B. fats, oils, waxes, silicones, emulsifiers, alcohols, polyols, thickeners, moisturizing and / or moisturizing substances, surfactants, plasticizers, foam retardants, anionic, cationic, nonionic or amphoteric polymers, alkalizing or acidifying agents, softeners, adsorbents, light stabilizers Electrolytes Sequestrants, organic solvents, preservatives, bactericides, antioxidants, vitamins, fragrances, flavors, sweeteners, colors and pigments.
Die erfindungsgemäßen kosmetischen und pharmazeutischen Zubereitungen liegen bei topischer Verabreichung vorteilhafterweise in Form einer flüssigen oder festen ÖI-in-Wasser-Emulsion, Wasser-in-ÖI-Emulsion, Mehrfach-Emulsion, Mikroemulsion, PIT-Emulsion oder Pickering-Emulsion, eines Hydrogels, eines alkhoholischen Gels, eines Lipogels, einer ein- oder mehrphasigen Lösung, eines Schaumes, einer Salbe, eines Pflasters, einer Suspension, eines Puders oder einer Mischung mit mindestens einem als medizinischen Klebstoff geeigneten Polymer vor. Die erfindungsgemäßen Hautbehandlungsmittel können auch in wasserfreier Form, wie beispielsweise einem Öl oder einem Balsam, dargereicht werden. Hierbei kann der Träger ein pflanzliches oder tierisches Öl, ein Mineralöl, ein synthetisches Öl oder eine Mischung solcher Öle sein.When applied topically, the cosmetic and pharmaceutical preparations according to the invention are advantageously in the form of a liquid or solid oil-in-water emulsion, water-in-oil emulsion, multiple emulsion, microemulsion, PIT emulsion or Pickering emulsion, a hydrogel, an alcoholic gel, a lipogel, a single or multi-phase solution, a foam, an ointment, a plaster, a suspension, a powder or a mixture with at least one polymer suitable as a medical adhesive. The skin treatment compositions according to the invention can also be administered in anhydrous form, such as, for example, an oil or a balm. The carrier can be a vegetable or animal oil, a mineral oil, a synthetic oil or a mixture of such oils.
Weiterhin können die erfindungsgemäßen Mittel als Mikroemulsion vorliegen . Unter Mikroemulsionen werden im Rahmen der Erfindung neben den thermodynamisch stabilen Mikroemulsionen auch die sogenannten "PIT"-Emulsionen verstanden. Bei diesen Emulsionen handelt es sich um Systeme mit den 3 Komponenten Wasser, Öl und Emulgator, die bei Raumtemperatur als ÖI-in-Wasser-Emulsion vorliegen. Beim Erwärmen dieser Systeme bilden sich in einem bestimmten Temperaturbereich (als Phaseninversiontemperatur oder "PIT" bezeichnet) Mikroemulsionen aus, die sich bei weiterer Erwärmung in Wasser-in-ÖI(W/O)-Emulsionen umwandeln. Bei anschließendem Abkühlen werden wieder O/W-Emulsionen gebildet, die aber auch bei Raumtemperatur als Mikroemulsionen oder als sehr feinteilige Emulsionen mit einem mittleren Teilchendurchmesser unter 400 nm und insbesondere von etwa 100-300 nm, vorliegen. Erfindungsgemäß können solche Mikro- oder "PIT"- Emulsionen bevorzugt sein, die einen mittleren Teilchendurchmesser von etwa 200 nm aufweisen. Einzelheiten bezüglich dieser "PIT-Emulsionen" z. B. der Druckschrift Angew. Chem. 97, 655 - 669 (1985) zu entnehmen. Die erfindungsgemäßen pharmazeutischen Zubereitungen werden neben topischer Anwendung auch auf enteralem, parenteralem oder rektalem Weg verabreicht. Für die Verabreichung auf enteralem Weg können die pharmazeutischen Zubereitungen in Form von Tabletten, Kapseln, Dragees, Sirupen, Suspensionen, Lösungen, Pulvern, Granulaten oder Emulsionen vorliegen. Für die Verabreichung auf parenteralem Weg können die Zubereitungen in Form von Lösungen oder Suspensionen zur Perfusion oder Injektion vorliegen. Für die Verabreichung auf rektalem Weg können die Zubereitungen in Form von Suppositorien vorliegen.The agents according to the invention can furthermore be present as a microemulsion. In the context of the invention, microemulsions are understood to mean not only the thermodynamically stable microemulsions but also the so-called “PIT” emulsions. These emulsions are systems with the 3 components water, oil and emulsifier, which are available as an oil-in-water emulsion at room temperature. When these systems are warmed up, microemulsions form in a certain temperature range (referred to as phase inversion temperature or "PIT"), which convert to water-in-oil (W / O) emulsions when heated further. Upon subsequent cooling, O / W emulsions are again formed, but these are also present at room temperature as microemulsions or as very fine-particle emulsions with an average particle diameter below 400 nm and in particular from about 100-300 nm. According to the invention, those micro- or "PIT" emulsions can be preferred which have an average particle diameter of approximately 200 nm. Details regarding these "PIT emulsions" e.g. B. the publication Angew. Chem. 97, 655-669 (1985). In addition to topical application, the pharmaceutical preparations according to the invention are also administered enterally, parenterally or rectally. For administration via the enteral route, the pharmaceutical preparations can be in the form of tablets, capsules, dragees, syrups, suspensions, solutions, powders, granules or emulsions. For parenteral administration, the preparations may be in the form of solutions or suspensions for perfusion or injection. The preparations can be in the form of suppositories for administration by the rectal route.
Die Wirkung der erfindungsgemäßen kosmetischen und pharmazeutischen Zubereitungen kann durch die geeignete Wahl der verwendeten Fettstoffe weiter optimiert werden. Geeignete Fettstoffe sind zum Beispiel:The effect of the cosmetic and pharmaceutical preparations according to the invention can be further optimized by the suitable choice of the fatty substances used. Suitable fat substances are for example:
- pflanzliche Öle, wie Sonnenblumenöl, Olivenöl, Sojaöl, Rapsöl, Mandelöl, Jojobaöl, Orangenöl, Weizenkeimöl, Pfirsichkernöl und die flüssigen Anteile des Kokosöls,vegetable oils, such as sunflower oil, olive oil, soybean oil, rapeseed oil, almond oil, jojoba oil, orange oil, wheat germ oil, peach seed oil and the liquid components of coconut oil,
- flüssige Paraffinöle, Isoparaffinöle und synthetische Kohlenwasserstoffe, z. B. 1 ,3-Di-(2-ethyl-hexyl)-cyclohexan (Cetiol® S) oder Polydecen,- liquid paraffin oils, isoparaffin oils and synthetic hydrocarbons, e.g. B. 1, 3-di- (2-ethyl-hexyl) cyclohexane (Cetiol ® S) or polydecene,
- Di-n-alkylether mit insgesamt 12 bis 36, insbesondere 12 bis 24 C-Atomen, z. B. Di-n-octylether (Cetiol® OE), Di-n- n-Hexyl-n-octylether und n-Octyl-n-decylether.- Di-n-alkyl ethers with a total of 12 to 36, in particular 12 to 24 carbon atoms, for. As di-n-octyl ether (Cetiol ® OE), di-n-n-hexyl-n-octyl ether and n-octyl-n-decyl ether.
- Fettsäuren, besonders lineare und/oder verzweigte, gesättigte und/oder ungesättigte C8-3o-Fettsäuren. Bevorzugt sind Cιo-22-Fettsäuren. Beispiele sind die Isostearinsäuren und Isopalmitinsäuren wie die unter der Handelsbezeichnung Edenor® vertriebenen Fettsäuren. Weitere typische Beispiele für solche Fettsäuren sind Capronsäure, Caprylsäure, 2-Ethylhexansäure, Caprinsäure, Laurinsäure, Isotridecansäure, Myristinsäure, Palmitinsäure, Palmitoleinsäure, Stearinsäure, Isostearinsäure, Ölsäure, Elaidinsäure, Petroselinsäure, Linolsäure, Linolensäure, Elaeostearinsäure, Arachidonsäure, Gadoleinsäure, Behensäure und Erucasäure sowie deren technische Mischungen. Besonders bevorzugt sind üblicherweise die Fettsäureschnitte, die aus Cocosöl oder Palmöl erhältlich sind; insbesondere bevorzugt ist der Einsatz von Stearinsäure. Fettalkohole, besonders gesättigte, ein- oder mehrfach ungesättigte, verzweigte oder unverzweigte Fettalkohole mit 6 - 30, bevorzugt 10 - 22 und ganz besonders bevorzugt 12 - 22 Kohlenstoffatomen. Einsetzbar im Sinne der Erfindung sind z. B. Decanol, Octanol, Octenol, Dodecenol, Decenol, Octadienol, Dodecadienol, Decadienol, Oleylalkohol, Erucaalkohol, Ricinolalkohol, Stearylalkohol, Isostearyl- alkohol, Cetylalkohol, Laurylalkohol, Myristylalkohol, Arachidylalkohol, Capryl- alkohol, Caprinalkohol, Linoleylalkohol, Linolenylalkohol und Behenylalkohol, sowie deren Guerbetalkohole, z. B. 2-Ethylhexanol, wobei diese Aufzählung beispielhaften und nicht limitierenden Charakter haben soll.- Fatty acids, especially linear and / or branched, saturated and / or unsaturated C 8 - 3 o-fatty acids. Cιo- 22 fatty acids are preferred. Examples are the isostearic acids and isopalmitic acids such as the fatty acids sold under the trade name Edenor ® . Further typical examples of such fatty acids are caproic acid, caprylic acid, 2-ethylhexanoic acid, capric acid, lauric acid, isotridecanoic acid, myristic acid, palmitic acid, palmitoleic acid, stearic acid, isostearic acid, oleic acid, elaidic acid, petroselinic acid, linoleic acid, linolenic acid, arenachidonic acid, gadachoic acid, gadachoic acid, gadolinic acid, gadachoic acid, gadachoic acid, gadachic acid, gaurachidic acid, gadic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid, gaic acidic acid and gaic acidic acid as well as their technical mixtures. The fatty acid cuts that are obtainable from coconut oil or palm oil are usually particularly preferred; the use of stearic acid is particularly preferred. Fatty alcohols, especially saturated, mono- or polyunsaturated, branched or unbranched fatty alcohols with 6 - 30, preferably 10 - 22 and very particularly preferably 12 - 22 carbon atoms. For the purposes of the invention, z. B. decanol, octanol, octenol, dodecenol, decenol, octadienol, dodecadienol, decadienol, oleyl alcohol, eruca alcohol, ricinol alcohol, stearyl alcohol, isostearyl alcohol, cetyl alcohol, lauryl alcohol, myristyl alcohol, arachidyl alcohol, linoleic alcohol, capryl alcohol, capryl alcohol as well as their Guerbet alcohols, e.g. B. 2-ethylhexanol, this list is intended to have exemplary and non-limiting character.
Esteröle, das heißt, Ester von C6-3o-Fettsäuren mit C2.30-Fettalkoholen. Bevorzugt sind die Monoester der Fettsäuren mit Alkoholen mit 2 bis 24 C- Atomen. Als Alkohol- und Säurekomponenten der Esteröle können die vorstehend genannten Substanzen verwendet werden. Erfindungsgemäß besonders bevorzugt sind Isopropylmyristat, lsononansäure-Cι6-i8-alkylester, 2-Ethylhexylpalmitat, Stearinsäure-2-ethylhexylester, Cetyloleat, Glycerin- tricaprylat, Kokosfettalkoholcaprinat/-caprylat, n-Butylstearat, Oleylerucat, Isopropylpalmitat, Oleyloleat, Laurinsäurehexylester, Di-n-butyladipat, Myristyl- myristat, Cetearyl Isononanoate und Ölsäuredecylester.Esteröle, that is, esters of C 6 - 3 o-fatty acids with C. 2 30 fatty alcohols. The monoesters of fatty acids with alcohols having 2 to 24 carbon atoms are preferred. The above-mentioned substances can be used as alcohol and acid components of the ester oils. According to the invention, particular preference is given to isopropyl myristate, isononanoic acid -C 6 -i 8 alkyl ester, 2-ethylhexyl palmitate, stearic acid 2-ethylhexyl ester, cetyl oleate, glycerol tricaprylate, coconut fatty alcohol caprinate / caprylate, n-butyl stearate, isopropyl enolate, oleylerolate ester, oleylerolate ester, oleylerucyl ester -n-butyl adipate, myristyl myristate, cetearyl isononanoate and oleic acid decyl ester.
Hydroxycarbonsäurealkylester, wobei die Vollester der Glycolsäure, Milchsäure, Äpfelsäure, Weinsäure oder Citronensäure bevorzugt sind, aber auch Ester der ß-Hydroxypropionsäure, der Tartronsäure, der D-Gluconsäure, Zuckersäure, Schleimsäure oder Glucuronsäure geeignet sind und besonders bevorzugt die Ester von Cι2-Cι5-Fettalkoholen, z. B. die Handelsprodukte Cosmacol® der EniChem, Augusta Industriale, sind,Hydroxycarboxylic acid alkyl esters, wherein the Vollester of glycolic acid, lactic acid, malic acid, tartaric acid or citric acid are preferred, but also esters of beta-hydroxypropionic acid, tartronic acid, D-gluconic acid, saccharic acid, mucic acid or glucuronic acid are suitable and particularly preferred are the esters of Cι 2 - Cι 5 fatty alcohols, for. B. are the commercial products Cosmacol ® from EniChem, Augusta Industriale,
Dicarbonsäureester wie Di-n-butyladipat, Di-(2-ethylhexyl)-adipat, Di-(2- ethylhexyl)-succinat und Di-isotridecyiacelaat sowie Diolester wie Ethylenglykoldioleat, Ethylenglykol-di-isotridecanoat, Propylenglykoldi(2- ethylhexanoat), Propylenglykol-di-isostearat, Propylenglykol-di-pelargonat, Butandiol-di-isostearat, Neopentylglykoldicaprylat, symmetrische, unsymmetrische oder cyclische Ester der Kohlensäure mitDicarboxylic acid esters such as di-n-butyl adipate, di- (2-ethylhexyl) adipate, di- (2-ethylhexyl) succinate and di-isotridecyiacelate as well as diol esters such as ethylene glycol dioleate, ethylene glycol di-isotridecanoate, propylene glycol di (2-ethylhexanoate), propylene glycol -di-isostearate, propylene glycol-di-pelargonate, butanediol-di-isostearate, neopentyl glycol dicaprylate, symmetrical, asymmetrical or cyclic esters of carbonic acid
Fettalkoholen, z. B. Glycerincarbonat oder Dicaprylylcarbonat (Cetiol® CC), - Mono,- Di- und Trifettsäureester von gesättigten und/oder ungesättigten linearen und/oder verzweigten Fettsäuren mit Glycerin, z. B. Monomuls® 90-O18, Monomuls® 90-L12 oder Cutina® MD,Fatty alcohols, e.g. B. glycerol carbonate or dicaprylyl carbonate (Cetiol ® CC), - Mono, - di- and trifatty acid esters of saturated and / or unsaturated linear and / or branched fatty acids with glycerin, e.g. B. Monomuls ® 90-O18, Monomuls ® 90-L12 or Cutina ® MD,
- Wachse, insbesondere Insektenwachse wie Bienenwachs und Hummelwachs, Pflanzenwachse wie Candelillawachs und Carnaubawachs, Fruchtwachse, Ozo- kerit, Mikrowachs, Ceresin, Paraffin, Triglyceride gesättigter und gegebenenfalls hydroxylierter Ci6-3o-Fettsäuren, wie z. B. gehärtete Triglyceridfette (hydriertes Palmöl, hydriertes Kokosöl, hydriertes Rizinusöl), Glyceryltribehenat oder Glyceryltri-12-hydroxystearat, synthetische Vollester aus Fettsäuren und Glykolen (z. B. Syncrowachs®) oder Polyolen mit 2 - 6 C-Atomen.- Waxes, in particular insect waxes such as beeswax and bumblebee wax, plant waxes such as candelilla wax and carnauba wax, fruit waxes, ozone kerit, micro waxes, ceresin, paraffin, triglycerides saturated and optionally hydroxylated Ci 6 - 3 o-fatty acids, such as. B. hardened triglyceride fats (hydrogenated palm oil, hydrogenated coconut oil, hydrogenated castor oil), glyceryl tribehenate or glyceryl tri-12-hydroxystearate, synthetic full esters of fatty acids and glycols (e.g. Syncrowachs ® ) or polyols with 2 - 6 C atoms.
- Siliconverbindungen, ausgewählt aus Decamethylcyclopentasiloxan, Dodeca- methylcyclohexasiloxan und Siliconpolymeren, die gewünschtenfalls quervernetzt sein können, z. B. Polydialkylsiloxane, Polyalkylarylsiloxane, ethoxylierte Poly- dialkylsiloxane, bevorzugt die Substanzen mit der INCI-Bezeichnung Dimethicone Copolyol, sowie Polydialkylsiloxane, die Amin- und/oder Hydroxy-Gruppen enthalten.- Silicone compounds selected from decamethylcyclopentasiloxane, dodecamethylcyclohexasiloxane and silicone polymers, which can, if desired, be cross-linked, e.g. B. polydialkylsiloxanes, polyalkylarylsiloxanes, ethoxylated polydialkylsiloxanes, preferably the substances with the INCI name Dimethicone Copolyol, and polydialkylsiloxanes containing amine and / or hydroxy groups.
Die Einsatzmenge der Fettstoffe beträgt 0, 1 - 50 Gew.%, bevorzugt 0,1 - 20 Gew.% und besonders bevorzugt 0,1 - 15 Gew.%, jeweils bezogen auf das gesamte Mittel.The amount of fatty substances used is 0.1 to 50% by weight, preferably 0.1 to 20% by weight and particularly preferably 0.1 to 15% by weight, in each case based on the total composition.
Die erfindungsgemäßen Hautbehandlungsmittel können weiterhin ein oder mehrere oberflächenaktive Substanzen als Emulgator oder Dispergiermittel enthalten. Emulgatoren bewirken an der Phasengrenzfläche die Ausbildung von wasser- bzw. ölstabilen Adsorptionsschichten, die die dispergierten Tröpfchen gegen Koaleszenz schützen und damit die Emulsion stabilisieren. Emulgatoren sind daher wie Tenside aus einem hydrophoben und einem hydrophilen Molekülteil aufgebaut. Hydrophile Emulgatoren bilden bevorzugt O/W - Emulsionen und hydrophobe Emulgatoren bilden bevorzugt W/O - Emulsionen. W/O-Emulsionen, die ohne hydrophile Emulgatoren stabilisiert sind, sind in den Offenlegungsschriften DE 19816665 A1 und DE 19801593 A1 offenbart. Unter einer Emulsion ist eine tröpfchenförmige Verteilung (Dispersion) einer Flüssigkeit in einer anderen Flüssigkeit unter Aufwand von Energie zur Schaffung von stabilisierenden Phasengrenzflächen mittels Tensiden zu verstehen. Die Auswahl dieser emulgierenden Tenside oder Emulgatoren richtet sich dabei nach den zu dispergierenden Stoffen und der jeweiligen äußeren Phase sowie der Feinteiligkeit der Emulsion.The skin treatment compositions according to the invention can furthermore contain one or more surface-active substances as an emulsifier or dispersant. Emulsifiers cause water or oil-stable adsorption layers to form at the phase interface, which protect the dispersed droplets against coalescence and thus stabilize the emulsion. Like surfactants, emulsifiers are therefore made up of a hydrophobic and a hydrophilic part of the molecule. Hydrophilic emulsifiers preferably form O / W emulsions and hydrophobic emulsifiers preferably form W / O emulsions. W / O emulsions which are stabilized without hydrophilic emulsifiers are disclosed in the published documents DE 19816665 A1 and DE 19801593 A1. Under an emulsion is a droplet-like distribution (dispersion) of a liquid in another liquid with the use of energy to create stabilizing phase interfaces Understand surfactants. The selection of these emulsifying surfactants or emulsifiers is based on the substances to be dispersed and the particular external phase as well as the fine particle size of the emulsion.
Erfindungsgemäß verwendbare Emulgatoren sind beispielsweiseEmulsifiers which can be used according to the invention are, for example
- Anlagerungsprodukte von 4 bis 30 Mol Ethylenoxid und/oder 0 bis 5 Mol Propylenoxid an lineare C8-C22-Fettalkohole, an Cι2-C22-Fettsäuren und an C8- Ci5-Alkylphenole,Addition products of 4 to 30 moles of ethylene oxide and / or 0 to 5 moles of propylene oxide with linear C 8 -C 22 fatty alcohols, with C 2 -C 22 fatty acids and with C 8 - Ci 5 alkylphenols,
- C-ι2-C22-Fettsäuremono- und -diester von Anlagerungsprodukten von 1 bis 30 Mol Ethylenoxid an C3-C6-Polyole, insbesondere an Glycerin,C 2 -C 22 fatty acid monoesters and diesters of addition products of 1 to 30 mol of ethylene oxide with C 3 -C 6 polyols, in particular with glycerol,
- Ethylenoxid- und Polyglycerin-Anlagerungsprodukte an Methylglucosid-Fettsäure- ester, Fettsäurealkanolamide und Fettsäureglucamide,- Ethylene oxide and polyglycerol adducts with methyl glucoside fatty acid esters, fatty acid alkanolamides and fatty acid glucamides,
- C8-C22-Alkylmono- und -oligoglycoside und deren ethoxylierte Analoga, wobei Oligomerisierungsgrade von 1 ,1 bis 5, insbesondere 1 ,2 bis 2,0, und Glucose als Zuckerkomponente bevorzugt sind,C 8 -C 22 alkyl mono- and oligoglycosides and their ethoxylated analogs, degrees of oligomerization of 1.1 to 5, in particular 1.2 to 2.0, and glucose as the sugar component being preferred,
- Gemische aus Alkyl-(oligo)-glucosiden und Fettalkoholen, z. B. das im Handel erhältliche Produkt Montanov®68,- Mixtures of alkyl (oligo) glucosides and fatty alcohols, e.g. B. the commercially available product Montanov ® 68,
- Anlagerungsprodukte von 5 bis 60 Mol Ethylenoxid an Rizinusöl und gehärtetes Rizinusöl,- adducts of 5 to 60 moles of ethylene oxide with castor oil and hardened castor oil,
- Partialester von Polyolen mit 3-6 Kohlenstoffatomen mit gesättigten C8-C2 - Fettsäuren,Partial esters of polyols with 3-6 carbon atoms with saturated C 8 -C 2 fatty acids,
- Sterole (Sterine). Als Sterole wird eine Gruppe von Steroiden verstanden, die am C-Atom 3 des Steroid-Gerüstes eine Hydroxylgruppe tragen und sowohl aus tierischem Gewebe (Zoosterole) wie auch aus pflanzlichen Fetten (Phytosterole) isoliert werden. Beispiele für Zoosterole sind das Cholesterol und das Lanosterol. Beispiele geeigneter Phytosterole sind Beta-Sitosterol, Stigmasterol, Campesterol und Ergosterol. Auch aus Pilzen und Hefen werden Sterole, die sogenannten Mykosterole, isoliert. - Phospholipide, vor allem die Glucose-Phospolipide, die z. B. als Lecithine bzw. Phosphatidylcholine aus z. B. Eidotter oder Pflanzensamen (z. B. Sojabohnen) gewonnen werden,- sterols. Sterols are understood to be a group of steroids which carry a hydroxyl group on the C atom 3 of the steroid structure and are isolated both from animal tissue (zoosterols) and from vegetable fats (phytosterols). Examples of zoosterols are cholesterol and lanosterol. Examples of suitable phytosterols are beta-sitosterol, stigmasterol, campesterol and ergosterol. Sterols, the so-called mycosterols, are also isolated from fungi and yeasts. - Phospholipids, especially the glucose phospholipids, which, for. B. as lecithins or phosphatidylcholines from z. B. egg yolk or plant seeds (e.g. soybeans) are obtained,
- Fettsäureester von Zuckern und Zuckeralkoholen wie Sorbit,Fatty acid esters of sugars and sugar alcohols such as sorbitol,
- Polyglycerine und Polyglycerinderivate, bevorzugt Polyglyceryl-2-dipolyhydroxy- stearat (Handelsprodukt Dehymuls® PGPH) und Polyglyceryl-3-diisostearat (Handelsprodukt Lameform® TGI),- polyglycerols and polyglycerol, preferably Polyglyceryl-2-dipolyhydroxy- stearate (commercial product Dehymuls ® PGPH) and polyglyceryl-3 diisostearate (Lameform ® TGI commercial product)
- Lineare und verzweigte C8-C3o-Fettsäuren und deren Na-, K-, Ammonium-, Ca-, Mg- und Zn - Salze.- Linear and branched C 8 -C 3 o fatty acids and their Na, K, ammonium, Ca, Mg and Zn salts.
Die erfindungsgemäßen kosmetischen und pharmazeutischen Zubereitungen enthalten die Emulgatoren bevorzugt in Mengen von 0,1 bis 25 Gew.-%, insbesondere 0,5 - 15 Gew.-%, bezogen auf das gesamte Mittel.The cosmetic and pharmaceutical preparations according to the invention preferably contain the emulsifiers in amounts of 0.1 to 25% by weight, in particular 0.5-15% by weight, based on the total composition.
Die erfindungsgemäßen Hautbehandlungsmittel können organische oder mineralische oder modifizierte mineralische Lichtschutzfilter enthalten. Bei den Lichtschutzfiltern handelt es sich um bei Raumtemperatur flüssig oder kristallin vorliegende Substanzen, die in der Lage sind, ultraviolette Strahlen zu absorbieren und die aufgenommene Energie in Form längerwelliger Strahlung, z. B. Wärme wieder abzugeben. Man unterscheidet UVA-Filter und UVB-Filter. Die UVA- und UVB-Filter können sowohl einzeln als auch in Mischungen eingesetzt werden. Der Einsatz von Filter-Mischungen ist erfindungsgemäß bevorzugt.The skin treatment agents according to the invention can contain organic or mineral or modified mineral light protection filters. The light protection filters are substances which are liquid or crystalline at room temperature and are able to absorb ultraviolet rays and absorb the energy in the form of longer-wave radiation, e.g. B. to release heat again. A distinction is made between UVA filters and UVB filters. The UVA and UVB filters can be used both individually and in mixtures. The use of filter mixtures is preferred according to the invention.
Die erfindungsgemäß verwendeten organischen UV-Filter sind ausgewählt aus den Derivaten von Dibenzoylmethan, Zimtsäureestern, Diphenylacrylsäureestern, Benzophenon, Campher, p-Aminobenzoesäureestern, o-Aminobenzoesäureestem, Salicylsäureestem, Benzimidazolen, 1 ,3,5-Triazinen, monomeren und oligomeren 4,4-Diarylbutadiencarbonsäureestern und -carbonsäureamiden,The organic UV filters used according to the invention are selected from the derivatives of dibenzoylmethane, cinnamic acid esters, diphenylacrylic acid esters, benzophenone, camphor, p-aminobenzoic acid esters, o-aminobenzoic acid esters, salicylic acid esters, benzimidazoles, 1, 3,5-triazines, monomeric and oligomeric 4,4- Diaryl butadiene carboxylic acid esters and carboxamides,
Ketotricyclo(5.2.1.0)decan, Benzalmalonsäureestern sowie beliebigen Mischungen der genannten Komponenten. Die organischen UV-Filter können öllöslich oder wasserlöslich sein. Erfindungsgemäß besonders bevorzugte öllösliche UV-Filter sind 1-(4-tert.-Butylphenyl)-3-(4'methoxyphenyl)propan-1 ,3-dion (Parsol® 1789), 1-Phenyl- 3-(4'-isopropylphenyl)-propan-1 ,3-dion, 3-(4'-Methylbenzyliden)-D,L-campher, 4- (Dimethylamino)-benzoesäure-2-ethylhexylester, 4-(Dimethylamino)benzoesäure-2- octylester, 4-(Dimethylamino)-benzoesäureamylester, 4-Methoxyzimtsäure-2- ethylhexylester, 4-Methoxyzimtsäurepropylester, 4-Methoxyzimtsäureisopentylester, 2-Cyano-3,3-phenylzimtsäure-2-ethylhexylester (Octocrylene), Salicylsäure-2-ethyl- hexylester, Salicylsäure-4-isopropylbenzylester, Salicylsäurehomomenthylester (3,3,5-Thmethyl-cyclohexylsalicylat), 2-Hydroxy-4-methoxybenzophenon, 2-Hydroxy- 4-methoxy-4'-methylbenzophenon, 2,2'-Dihydroxy-4-methoxybenzophenon, 4- Methoxybenzmalonsäuredi-2-ethylhexylester, 2,4,6-Trianilino-(p-carbo-2'-ethyl-1 '- hexyloxy)-1 ,3,5-thazin (Octyl Triazone) und Dioctyl Butamido Triazone (Uvasorb® HEB) sowie beliebige Mischungen der genannten Komponenten.Ketotricyclo (5.2.1.0) decane, benzalmalonic acid esters and any mixtures of the components mentioned. The organic UV filters can be oil-soluble or water-soluble. Oil-soluble UV filters which are particularly preferred according to the invention 1- (4-tert-butylphenyl) -3- (4'methoxyphenyl) propane-1, 3-dione (Parsol ® 1789), 1-phenyl-3- (4'-isopropylphenyl) -propane-1, 3- dione, 3- (4 ' -methylbenzylidene) -D, L-camphor, 4- (dimethylamino) -benzoic acid 2-ethylhexyl ester, 4- (dimethylamino) benzoic acid-2-octyl ester, 4- (dimethylamino) -benzoic acid amyl ester, 4- 2-ethylhexyl methoxycinnamate, propyl 4-methoxycinnamate, isopentyl 4-methoxycinnamate, 2-ethylhexyl 2-cyano-3,3-phenylcinnamate (octocrylene), 2-ethylhexyl salicylate, 4-isopropylbenzyl salicylate, salicylic acid ester , 5-methyl-cyclohexyl salicylate), 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxy-4'-methylbenzophenone, 2,2'-dihydroxy-4-methoxybenzophenone, 4-methoxybenzmalonic acid di-2-ethylhexyl ester, 2, 4,6-Trianilino- (p-carbo-2'-ethyl-1 '- hexyloxy) -1, 3,5-thazine (octyl triazone) and dioctyl butamido triazone (Uvasorb ® HEB) as well as any mixtures of the components mentioned.
Bevorzugte wasserlösliche UV-Filter sind 2-Phenylbenzimidazol-5-sulfonsäure und deren Alkali-, Erdalkali-, Ammonium-, Alkylammonium-, Alkanolammonium- und Glucammoniumsalze, Sulfonsäurederivate von Benzophenonen, vorzugsweise 2- Hydroxy-4-methoxybenzophenon-5-sulfonsäure und ihre Salze, Sulfonsäurederivate des 3-Benzylidencamphers, wie z. B. 4-(2-Oxo-3-bomylidenmethyl) benzolsulfonsäure und 2-Methyl-5-(2-oxo-3-bornyliden)sulfonsäure und deren Salze.Preferred water-soluble UV filters are 2-phenylbenzimidazole-5-sulfonic acid and its alkali, alkaline earth, ammonium, alkylammonium, alkanolammonium and glucammonium salts, sulfonic acid derivatives of benzophenones, preferably 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid and their Salts, sulfonic acid derivatives of 3-benzylidene camphor, such as. B. 4- (2-oxo-3-bomylidenemethyl) benzenesulfonic acid and 2-methyl-5- (2-oxo-3-bornylidene) sulfonic acid and their salts.
Bei den erfindungsgemäß bevorzugten anorganischen Lichtschutzpigmenten handelt es sich um feindisperse Metalloxide und Metallsalze, beispielsweise Titandioxid, Zinkoxid, Eisenoxid, Aluminiumoxid, Ceroxid, Zirkoniumoxid, Silicate (Talk), Bariumsulfat und Zinkstearat. Die Partikel sollten dabei einen mittleren Durchmesser von weniger als 100 nm, vorzugsweise zwischen 5 und 50 nm und insbesondere zwischen 15 und 30 nm aufweisen. Sie können eine sphärische Form aufweisen, es können jedoch auch solche Partikel zum Einsatz kommen, die eine ellipsoide oder in sonstiger Weise von der sphärischen Gestalt abweichende Form besitzen. Die Pigmente können auch oberflächenbehandelt, d.h. hydrophilisiert oder hydrophobiert vorliegen. Typische Beispiele sind gecoatete Titandioxide, wie z. B. Titandioxid T 805 (Degussa) oder Eusolex® T2000 (Merck). Als hydrophobe Coatingmittel kommen dabei vor allem Silicone und dabei speziell Trialkoxyoctylsilane oder Simethicone in Frage. In Sonnenschutzmitteln werden bevorzugt sogenannte Mikro- oder Nanopigmente eingesetzt. Vorzugsweise wird mikronisiertes Zinkoxid verwendet.The preferred inorganic light protection pigments according to the invention are finely dispersed metal oxides and metal salts, for example titanium dioxide, zinc oxide, iron oxide, aluminum oxide, cerium oxide, zirconium oxide, silicates (talc), barium sulfate and zinc stearate. The particles should have an average diameter of less than 100 nm, preferably between 5 and 50 nm and in particular between 15 and 30 nm. They can have a spherical shape, but it is also possible to use particles which have an ellipsoidal shape or a shape which differs from the spherical shape in some other way. The pigments can also be surface-treated, ie hydrophilized or hydrophobicized. Typical examples are coated titanium dioxide, such as. B. Titanium dioxide T 805 (Degussa) or Eusolex ® T2000 (Merck). Silicones, and in particular trialkoxyoctylsilanes or simethicones, are particularly suitable as hydrophobic coating agents Question. So-called micro- or nanopigments are preferably used in sunscreens. Micronized zinc oxide is preferably used.
Weiterhin können die erfindungsgemäßen HautbehandlungsmittelFurthermore, the skin treatment agents according to the invention
Proteinhydrolysate oder deren Derivat enthalten. Erfindungsgemäß können sowohl pflanzliche als auch tierische Proteinhydrolysate eingesetzt werden. Tierische Proteinhydrolysate sind z. B. Elastin-, Collagen-, Keratin-, Seiden- und Milcheiweiß- Proteinhydrolysate, die auch in Form von Salzen vorliegen können. Erfindungsgemäß bevorzugt sind pflanzliche Proteinhydrolysate, z. B. Soja-, Weizen-, Mandel-, Erbsen-, Kartoffel- und Reisproteinhydrolysate. Entsprechende Handelsprodukte sind z. B. DiaMin® (Diamalt), Gluadin® (Cognis), Lexein® (Inolex) und Crotein® (Croda).Contain protein hydrolyzates or their derivatives. According to the invention, both vegetable and animal protein hydrolyzates can be used. Animal protein hydrolyzates are e.g. B. elastin, collagen, keratin, silk and milk protein protein hydrolyzates, which may also be in the form of salts. Vegetable protein hydrolyzates, e.g. B. soy, wheat, almond, pea, potato and rice protein hydrolyzates. Corresponding commercial products are e.g. B. DiaMin ® (Diamalt), Gluadin ® (Cognis), Lexein ® (Inolex) and Crotein ® (Croda).
Wenngleich der Einsatz der zusätzlichen Proteinhydrolysate als solche bevorzugt ist, können an ihrer Stelle gegebenenfalls auch anderweitig erhaltene Aminosäuregemische oder einzelne Aminosäuren wie beispielsweise Arginin, Lysin, Histidin oder Pyrroglutaminsäure eingesetzt werden. Ebenfalls möglich ist der Einsatz von Derivaten der Proteinhydrolysate, z. B. in Form ihrer Fettsäure- Kondensationsprodukte. Entsprechende Handelsprodukte sind z. B. Lamepon® (Cognis), Gluadin® (Cognis), Lexein® (Inolex), Crolastin® oder Crotein® (Croda).Although the use of the additional protein hydrolyzates as such is preferred, amino acid mixtures or individual amino acids, such as arginine, lysine, histidine or pyrroglutamic acid, which have been obtained in some other way can also be used instead of them. It is also possible to use derivatives of protein hydrolyzates, e.g. B. in the form of their fatty acid condensation products. Corresponding commercial products are e.g. B. Lamepon ® (Cognis), Gluadin ® (Cognis), Lexein ® (Inolex), Crolastin ® or Crotein ® (Croda).
In den erfindungsgemäßen kosmetischen und pharmazeutischen Zubereitungen sind die zusätzlichen Proteinhydrolysate und deren Derivate in Mengen von 0,01 - 10 Gew.-% bezogen auf das gesamte Mittel enthalten. Mengen von 0,1 bis 5 Gew.%, insbesondere 0,1 bis 3 Gew.-%, sind besonders bevorzugt.The cosmetic and pharmaceutical preparations according to the invention contain the additional protein hydrolyzates and their derivatives in amounts of 0.01-10% by weight, based on the total composition. Amounts of 0.1 to 5% by weight, in particular 0.1 to 3% by weight, are particularly preferred.
Weiterhin können die erfindungsgemäßen Hautbehandlungsmittel Mono-, Oligo- oder Polysaccharide oder deren Derivate enthalten.The skin treatment compositions according to the invention can furthermore contain mono-, oligo- or polysaccharides or their derivatives.
Erfindungsgemäß geeignete Monosaccharide sind z. B. Glucose, Fructose, Galactose, Arabinose, Ribose, Xylose, Lyxose, Aliose, Altrose, Mannose, Gulose, Idose und Talose, die Desoxyzucker Fucose und Rhamnose sowie Aminozucker wie z. B. Glucosamin oder Galactosamin. Bevorzugt sind Glucose, Fructose, Galactose, Arabinose und Fucose; Glucose ist besonders bevorzugt.Suitable monosaccharides according to the invention are e.g. B. glucose, fructose, galactose, arabinose, ribose, xylose, lyxose, aliases, old rose, mannose, gulose, idose and talose, the deoxy sugar fucose and rhamnose and amino sugar such as z. B. glucosamine or galactosamine. Glucose, fructose, galactose, arabinose and fucose are preferred; Glucose is particularly preferred.
Erfindungsgemäß geeignete Oligosaccharide sind aus zwei bis zehn Monosaccharid- einheiten zusammengesetzt, z. B. Saccharose, Lactose oder Trehalose. Ein besonders bevorzugtes Oligosaccharid ist Saccharose. Ebenfalls besonders bevorzugt ist die Verwendung von Honig, der überwiegend Glucose und Saccharose enthält.Suitable oligosaccharides according to the invention are composed of two to ten monosaccharide units, for. B. sucrose, lactose or trehalose. A particularly preferred oligosaccharide is sucrose. The use of honey, which predominantly contains glucose and sucrose, is also particularly preferred.
Erfindungsgemäß geeignete Polysaccharide sind aus mehr als zehn Monosaccharid- einheiten zusammengesetzt. Bevorzugte Polysaccharide sind die aus α-D-Glucose- Einheiten aufgebauten Stärken sowie Stärkeabbauprodukte wie Amylose, Amylo- pektin und Dextrine. Erfindungsgemäß besonders vorteilhaft sind chemisch und/oder thermisch modifizierte Stärken, z. B. Hydroxypropylstärkephosphat, Dihydroxypropyldistärkephosphat oder die Handelsprodukte Dry Flo®. Weiterhin bevorzugt sind Dextrane sowie ihre Derivate, z. B. Dextransulfat. Ebenfalls bevorzugt sind nichtionische Cellulose-Derivate, wie Methylcellulose, Hydroxypropylcellulose oder Hydroxyethylcellulose, sowie kationische Cellulose-Derivate, z. B. die Handelsprodukte Celquat® und Polymer JR®, und bevorzugt Celquat® H 100, Celquat® L 200 und Polymer JR® 400 (Polyquaternium-10) sowie Polyquaternium-24. Weitere bevorzugte Beispiele sind Polysaccharide aus Fucose-Einheiten, z. B. das Handelsprodukt Fucogel®. Besonders bevorzugt sind die aus Aminozuckereinheiten aufgebauten Polysaccharide, insbesondere Chitine und ihre deacetylierten Derivate, die Chito- sane, und Mucopolysaccharide. Zu den erfindungsgemäß bevorzugten Mucopoly- sacchariden gehören Hyaluronsäure und ihre Derivate, z. B. Natriumhyaluronat oder Dimethylsilanolhyaluronat, sowie Chondroitin und seine Derivate, z. B. Chondroitin- sulfat.Polysaccharides suitable according to the invention are composed of more than ten monosaccharide units. Preferred polysaccharides are the starches made up of α-D-glucose units and starch degradation products such as amylose, amylopectin and dextrins. Chemically and / or thermally modified starches, eg. B. hydroxypropyl starch phosphate, dihydroxypropyl distarch phosphate or the commercial products Dry Flo ® . Dextrans and their derivatives, e.g. B. dextran sulfate. Also preferred are nonionic cellulose derivatives, such as methyl cellulose, hydroxypropyl cellulose or hydroxyethyl cellulose, and cationic cellulose derivatives, e.g. B. the commercial products Celquat ® and Polymer JR ® , and preferably Celquat ® H 100, Celquat ® L 200 and Polymer JR ® 400 (Polyquaternium-10) and Polyquaternium-24. Further preferred examples are polysaccharides from fucose units, e.g. B. the commercial product Fucogel ® . The polysaccharides composed of amino sugar units, in particular chitins and their deacetylated derivatives, the chitosans and mucopolysaccharides, are particularly preferred. The preferred mucopoly saccharides according to the invention include hyaluronic acid and its derivatives, e.g. B. sodium hyaluronate or dimethylsilanol hyaluronate, and chondroitin and its derivatives, e.g. B. chondroitin sulfate.
Die erfindungsgemäßen kosmetischen und pharmazeutischen Zubereitungen können weitere Pflanzenextrakte enthalten. Sie werden üblicherweise durch Extraktion der gesamten Pflanze, in einzelnen Fällen aber auch ausschließlich aus Blüten und/oder Blättern und/oder Samen und/oder anderen Pflanzenteilen, her- gestellt. Erfindungsgemäß sind vor allem die Extrakte aus dem Meristem, also dem teilungsfähigen Bildungsgewebe der Pflanzen, und speziellen Pflanzen wie Grünem Tee, Hamamelis, Kamille, Ringelblume, Paeonie, Aloe Vera, Rosskastanie, Salbei, Weidenrinde, Weißdorn, Lindenblüten, Mandeln, Fichtennadeln, Sandelholz, Kokosnuß, Kiwi, Guave, Limette, Mango, Aprikose, Weizen, Melone, Orange, Grapefruit, Avocado, Rosmarin, Malve, Wiesenschaumkraut, Thymian, Melisse, Eibisch (Althaea), Malve (Malva sylvestris), Ginseng, Maiglöckchen und Süßkartoffel bevorzugt. Vorteilhaft eingesetzt werden können auch Algenextrakte. Die erfindungsgemäß verwendeten Algenextrakte stammen aus Grünalgen, Braunalgen, Rotalgen oder Blaualgen (Cyanobakterien). Die zur Extraktion eingesetzten Algen können sowohl natürlichen Ursprungs als auch durch biotechnologische Prozesse gewonnen und gewünschtenfalls gegenüber der natürlichen Form verändert sein. Die Veränderung der Organismen kann gentechnisch, durch Züchtung oder durch die Kultivation in mit ausgewählten Nährstoffen angereicherten Medien erfolgen. Bevorzugte Algenextrakte stammen aus Seetang, Blaualgen, aus der Grünalge Codium tomentosum sowie aus der Braunalge Fucus vesiculosus. Ein besonders bevorzugter Algenextrakt stammt aus Blaualgen der Species Spirulina, die in einem Magnesium-angereicherten Medium kultiviert wurden.The cosmetic and pharmaceutical preparations according to the invention can contain further plant extracts. They are usually obtained by extracting the entire plant, but in individual cases also exclusively from flowers and / or leaves and / or seeds and / or other parts of plants. posed. According to the invention, the extracts from the meristem, i.e. the divisible educational tissue of the plants, and special plants such as green tea, witch hazel, chamomile, calendula, peony, aloe vera, horse chestnut, sage, willow bark, hawthorn, linden flowers, almonds, spruce needles, sandalwood , Coconut, kiwi, guava, lime, mango, apricot, wheat, melon, orange, grapefruit, avocado, rosemary, mallow, cuckoo flower, thyme, lemon balm, marshmallow (Althaea), mallow (Malva sylvestris), ginseng, lily of the valley and sweet potato are preferred , Algae extracts can also be used to advantage. The algae extracts used according to the invention come from green algae, brown algae, red algae or blue-green algae (cyanobacteria). The algae used for the extraction can be of natural origin as well as obtained through biotechnological processes and, if desired, can be changed compared to the natural form. The organisms can be changed genetically, by breeding or by cultivation in media enriched with selected nutrients. Preferred algae extracts come from seaweed, blue-green algae, from the green algae Codium tomentosum and from the brown algae Fucus vesiculosus. A particularly preferred algae extract comes from blue-green algae of the Spirulina species, which were cultivated in a magnesium-enriched medium.
Besonders bevorzugt sind die Extrakte aus Spirulina, Grünem Tee, Aloe Vera, Meristem, Hamamelis, Aprikose, Ringelblume, Guave, Süßkartoffel, Limette, Mango, Kiwi, Gurke, Malve, Eibisch und Veilchen. Die erfindungsgemäßen kosmetischen und pharmazeutischen Zubereitungen können auch Mischungen aus mehreren, insbesondere aus zwei, verschiedenen Pflanzenextrakten enthalten.The extracts from spirulina, green tea, aloe vera, meristem, witch hazel, apricot, marigold, guava, sweet potato, lime, mango, kiwi, cucumber, mallow, marshmallow and violet are particularly preferred. The cosmetic and pharmaceutical preparations according to the invention can also contain mixtures of several, in particular two, different plant extracts.
Die erfindungsgemäßen kosmetischen und pharmazeutischen Zubereitungen können weitere Wirk-, Hilfs- und Zusatzstoffe enthalten, beispielsweise:The cosmetic and pharmaceutical preparations according to the invention can contain further active ingredients, auxiliaries and additives, for example:
- Vitamine, Provitamine und Vitaminvorstufen aus den Gruppen A, C, E und F, insbesondere Retinol (Vitamin Ai) sowie seine Ester, z.B. das Acetat und dasVitamins, provitamins and vitamin precursors from groups A, C, E and F, in particular retinol (vitamin Ai) and its esters, e.g. the acetate and the
Palmitat, 3,4-Didehydroretinol (Vitamin A2), ß-Carotin (Provitamin des VitaminPalmitate, 3,4-didehydroretinol (vitamin A 2 ), ß-carotene (provitamin of the vitamin
Ai), Ascorbinsäure (Vitamin C), sowie die Palmitinsäureester, Glucoside oderAi), ascorbic acid (vitamin C), and the palmitic acid esters, glucosides or
Phosphate der Ascorbinsäure, Tocopherole, insbesondere -Tocopherol sowie seine Ester, z. B. das Acetat, das Nicotinat, das Phosphat und das Succinat; weiterhin Vitamin F, worunter essentielle Fettsäuren, besonders Linolsäure, Linolensäure und Arachidonsäure, verstanden werden;Phosphates of ascorbic acid, tocopherols, especially tocopherol and its esters, e.g. B. the acetate, nicotinate, phosphate and succinate; also vitamin F, which is understood to mean essential fatty acids, in particular linoleic acid, linolenic acid and arachidonic acid;
Allantoin,allantoin,
Bisabolol,bisabolol,
Antioxidantien, zum Beispiel Aminosäuren (z. B. Glycin, Histidin, Tyrosin, Tryp- tophan) und deren Derivate, Imidazole (z. B. Urocaninsäure) und deren Derivate, Peptide wie D,L-Carnosin, D-Carnosin, L-Carnosin und deren Derivate (z. B. Anserin), Chlorogensäure und deren Derivate, Liponsäure und deren Derivate (z. B. Dihydroliponsäure), Aurothioglucose, Propylthiouracil und andere Thiole (z. B. Thioredoxin, Glutathion, Cystein, Cystin, Cystamin und deren Glycosyl-, N- Acetyl-, Methyl-, Ethyl-, Propyl-, Amyl-, Butyl- und Lauryl-, Palmitoyl-, Oleyl-, γ-Linoleyl-, Cholesteryl- und Glycerylester) sowie deren Salze, Dilaurylthiodipropionat, Distearylthiodipropionat, Thiodipropionsäure und deren Derivate (Ester, Ether, Peptide, Lipide, Nukieotide, Nukleoside und Salze) sowie Sulfoximinverbindungen (z. B. Buthioninsulfoximine, Homocysteinsulfoximin, Bu- tioninsulfone, Penta-, Hexa-, Heptathioninsulfoximin) in sehr geringen verträglichen Dosierungen (z. B. pmol bis μmol/kg), ferner (Metall)-Chelatoren (z. B. α-Hydroxyfettsäuren, Palmitinsäure, Phytinsäure, Lactoferrin), Huminsäure, Gallensäure, Gallenextrakte, Bilirubin, Biliverdin, EDTA, EGTA und deren Derivate, ungesättigte Fettsäuren und deren Derivate (z. B. γ-Linolensäure, Linolsäure, Ölsäure), Folsäure und deren Derivate, Ubichinon und Ubichinol und deren Derivate, das Koniferylbenzoat des Benzoeharzes, Rutinsäure und deren Derivate, α-Glycosylrutin, Ferulasäure, Furfurylidenglucitol, Carnosin, Butylhydro- xytoluol, Butylhydroxyanisol, Nordihydroguajakharzsäure, Nordihydro- guajaretsäure, Trihydroxybutyrophenon, Harnsäure und deren Derivate, Katalase, Superoxid-Dismutase, Zink und dessen Derivate (z. B. ZnO, ZnSO4), Selen und dessen Derivate (z. B. Selen-Methionin), Stilbene und deren Derivate (z. B. Stilbenoxid, trans-Stilbenoxid) und die als Antioxidans geeigneten Derivate (Salze, Ester, Ether, Zucker, Nukieotide, Nukleoside, Peptide und Lipide) dieser Wirkstoffe,Antioxidants, for example amino acids (e.g. glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (e.g. urocanic acid) and their derivatives, peptides such as D, L-carnosine, D-carnosine, L- Carnosine and its derivatives (e.g. anserine), chlorogenic acid and its derivatives, lipoic acid and its derivatives (e.g. dihydroliponic acid), aurothioglucose, propylthiouracil and other thiols (e.g. thioredoxin, glutathione, cysteine, cystine, cystamine and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl, γ-linoleyl, cholesteryl and glyceryl esters) and their salts, dilauryl thiodipropionate, distearyl thiodipropionate , Thiodipropionic acid and its derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts) as well as sulfoximine compounds (e.g. buthionine sulfoximines, homocysteine sulfoximine, butionic sulfones, penta-, hexa-, heptathione sulfoximine) in very low tolerable doses (e.g. B. pmol to μmol / kg), further (Me tall) chelators (e.g. B. α-hydroxy fatty acids, palmitic acid, phytic acid, lactoferrin), humic acid, bile acid, bile extracts, bilirubin, biliverdin, EDTA, EGTA and their derivatives, unsaturated fatty acids and their derivatives (e.g. γ-linolenic acid, linoleic acid, oleic acid), folic acid and their derivatives, ubiquinone and ubiquinol and their derivatives, the coniferyl benzoate of benzoin, rutinic acid and their derivatives, α-glycosylrutin, ferulic acid, furfurylidene glucitol, carnosine, butylhydroxy toluene, butylhydroxyanisole, nordihydroguajyrobenzoic acid, nordarydroxybenzydroxybenzoic acid, nordihetsyrenic acid, nordihetsyrenic acid, nordihetsyrenic acid, nordihetsyrenic acid, nordihetsyrenic acid, nordihetsyrenic acid, nordihetsyrenic acid; Catalase, superoxide dismutase, zinc and its derivatives (e.g. ZnO, ZnSO 4 ), selenium and its derivatives (e.g. selenium methionine), stilbenes and their derivatives (e.g. stilbene oxide, trans-stilbene oxide) and the derivatives suitable as antioxidants (salts, esters, ethers, sugars, nucleotides, nucleosides, peptides and lipids) of these active ingredients,
Ceramide und Pseudoceramide, - Triterpene, insbesondere Triterpensäuren wie Ursolsäure, Rosmarinsäure, Betulinsäure, Boswelliasäure und Bryonolsäure,Ceramides and pseudoceramides, Triterpenes, especially triterpenic acids such as ursolic acid, rosmaric acid, betulinic acid, boswellic acid and bryonolic acid,
- Monomere Catechine, besonders Catechin und Epicatechin, Leukoanthocyanidine, Catechinpolymere (Catechin-Gerbstoffe) sowie Gallotannine,Monomeric catechins, especially catechin and epicatechin, leucoanthocyanidins, catechin polymers (catechin tannins) and gallotannins,
- Verdickungsmittel, z. B. Gelatine, Pflanzengumme wie Agar-Agar, Guar-Gum, Alginate, Xanthan-Gum, Gummi arabicum, Karaya-Gummi oder Johannisbrotkernmehl, natürliche und synthetische Tone und Schichtsilikate, z. B. Bentonit, Hectorit, Montmorillonit oder Laponite®, vollsynthetische Hydrokolloide wie z. B. Polyvinylalkohol, und außerdem Ca-, Mg- oder Zn-Seifen von Fettsäuren,- Thickeners, e.g. B. gelatin, vegetable gums such as agar agar, guar gum, alginates, xanthan gum, gum arabic, karaya gum or locust bean gum, natural and synthetic clays and layered silicates, e.g. B. bentonite, hectorite, montmorillonite or Laponite ® , fully synthetic hydrocolloids such. B. polyvinyl alcohol, and also Ca, Mg or Zn soaps of fatty acids,
Pflanzenglycoside,plant glycosides,
Strukturanten wie Maleinsäure und Milchsäure,Structurants such as maleic acid and lactic acid,
Dimethylisosorbid,dimethyl isosorbide,
- Alpha-, beta- sowie gamma-Cyclodextrine, insbesondere zur Stabilisierung von Retinol,Alpha, beta and gamma cyclodextrins, in particular for stabilizing retinol,
Lösungsmittel, Quell- und Penetrationsstoffe wie Ethanol, Isopropanol, Ethylenglykol, Propylenglykol, Propylenglykolmonoethylether, Glycerin und Diethylenglykol, Carbonate, Hydrogencarbonate, Guanidine, Harnstoffe sowie primäre, sekundäre und tertiäre PhosphateSolvents, swelling and penetration substances such as ethanol, isopropanol, ethylene glycol, propylene glycol, propylene glycol monoethyl ether, glycerin and diethylene glycol, carbonates, hydrogen carbonates, guanidines, ureas and primary, secondary and tertiary phosphates
Parfümöle, Pigmente sowie Farbstoffe zum Anfärben des Mittels,Perfume oils, pigments and dyes for coloring the agent,
Substanzen zur Einstellung des pH-Wertes, z. B. α- und ß-Hydroxycarbonsäuren,Substances for adjusting the pH, e.g. B. α- and ß-hydroxycarboxylic acids,
Komplexbildner wie EDTA, NTA, ß-Alanindiessigsäure und Phosphonsäuren,Complexing agents such as EDTA, NTA, ß-alaninediacetic acid and phosphonic acids,
- Trübungsmittel wie Latex, Styrol/PVP- und Styrol/Acrylamid-Copolymere, Perlglanzmittel wie Ethyienglykolmono- und -distearat sowie PEG-3-distearat,Opacifiers such as latex, styrene / PVP and styrene / acrylamide copolymers, pearlescent agents such as ethylene glycol mono- and distearate and PEG-3 distearate,
- Treibmittel wie Propan-Butan-Gemische, N2O, Dimethylether, CO2 und Luft.- Blowing agents such as propane-butane mixtures, N 2 O, dimethyl ether, CO 2 and air.
Die erfindungsgemäßen Hautbehandlungsmittel können ein oder mehrere filmbildende, emulsionsstabilisierende, verdickende oder adhäsive Polymere, ausgewählt aus natürlichen und synthetischen Polymeren, die kationisch, anionisch, amphoter geladen oder nichtionisch sein können, enthalten.The skin treatment agents according to the invention can contain one or more film-forming, emulsion-stabilizing, thickening or adhesive polymers, selected from natural and synthetic polymers, which can be cationic, anionic, amphoteric or non-ionic.
Erfindungsgemäß bevorzugt sind kationische, anionische sowie nichtionischeCationic, anionic and nonionic are preferred according to the invention
Polymere.Polymers.
Unter den kationischen Polymeren bevorzugt sind Polysiloxane mit quaternären Gruppen, z. B. die Handelsprodukte Q2-7224 (Dow Corning), Dow Corning® 929 Emulsion (mit Amodimethicone), SM-2059 (General Electric), SLM-55067 (Wacker) sowie Abil®-Quat 3270 und 3272 (Th. Goldschmidt).Preferred among the cationic polymers are polysiloxanes with quaternary groups, e.g. B. the commercial products Q2-7224 (Dow Corning), Dow Corning ® 929 emulsion (with Amodimethicone), SM-2059 (General Electric), SLM-55067 (Wacker) and Abil ® -Quat 3270 and 3272 (Th. Goldschmidt).
Bevorzugte anionische Polymere, die die Wirkung des erfindungsgemäß verwendeten Wirkstoffs unterstützen können, enthalten Carboxylat- und/oder Sulfonatgruppen und als Monomere zum Beispiel Acrylsäure, Methacrylsäure, Crotonsäure, Maleinsäureanhydrid und 2-Acrylamido-2-methylpropansulfonsäure. Dabei können die sauren Gruppen ganz oder teilweise als Natrium-, Kalium-, Ammonium-, Mono- oder Triethanolammonium-Salz vorliegen. Bevorzugte Monomere sind 2-Acrylamido-2-methylpropansulfonsäure und Acrylsäure. Ganz besonders bevorzugte anionische Polymere enthalten als alleiniges Monomer oder als Comonomer 2-Acrylamido-2-methylpropansulfonsäure, wobei die Sulfonsäure- gruppe ganz oder teilweise in Salzform vorliegen kann. Innerhalb dieser Ausführungsform ist es bevorzugt, Copolymere aus mindestens einem anionischen Monomer und mindestens einem nichtionischen Monomer einzusetzen. Bezüglich der anionischen Monomere wird auf die oben aufgeführten Substanzen verwiesen. Bevorzugte nichtionogene Monomere sind Acrylamid, Methacrylamid, Acrylsäureester, Methacrylsäureester, Vinylpyrrolidon, Vinylether und Vinylester. Bevorzugte anionische Copolymere sind Acrylsäure-Acrylamid-Copolymere sowie insbesondere Polyacrylamidcopolymere mit Sulfonsäuregruppen-haltigen Monomeren. Ein besonders bevorzugtes anionisches Copolymer besteht aus 70 bis 55 Mol-% Acrylamid und 30 bis 45 Mol-% 2-Acrylamido-2-methylpropansulfonsäure, wobei die Sulfonsäuregruppen ganz oder teilweise als Natrium-, Kalium-, Ammonium-, Mono- oder Triethanolammonium-Salz vorliegen. Dieses Copolymer kann auch vernetzt vorliegen, wobei als Vernetzungsagentien bevorzugt polyolefinisch ungesättigte Verbindungen wie Tetraallyloxyethan, Allylsucrose, Allylpentaerythrit und Methylen-bisacrylamid zum Einsatz kommen. Ein solches Polymer ist in dem Handelsprodukt Sepigel®305 der Firma SEPPIC enthalten. Die Verwendung dieses Compounds hat sich im Rahmen der erfindungsgemäßen Lehre als besonders vorteilhaft erwiesen. Auch die unter der Bezeichnung Simulgel®600 als Compound mit Isohexadecan und Polysorbat-80 vertriebenen Natriumacryloyldimethyltaurat-Copoly- mere haben sich als erfindungsgemäß besonders wirksam erwiesen. Weitere besonders bevorzugte anionische Homo- und Copolymere sind unvernetzte und vernetzte Polyacrylsäuren. Dabei können Allylether von Pentaerythrit, von Sucrose und von Propylen bevorzugte Vernetzungsagentien sein. Solche Verbindungen sind zum Beispiel die Handelsprodukte Carbopol®. Ein besonders bevorzugtes anionisches Copolymer enthält als Monomer zu 80 - 98 % eine ungesättigte, gewünschtenfalls substituierte C3.6-Carbonsäure oder ihr Anhydrid sowie zu 2 - 20 % gewünschtenfalls substituierte Acrylsäureester von gesättigten C-ιo-30-Carbonsäuren, wobei das Copolymer mit den vorgenannten Vernetzungsagentien vernetzt sein kann. Entsprechende Handelsprodukte sind Pemulen® und die Carbopol®-Typen 954, 980, 1342 und ETD 2020 (ex B.F. Goodrich).Preferred anionic polymers which can support the action of the active ingredient used according to the invention contain carboxylate and / or sulfonate groups and, for example, acrylic acid, methacrylic acid, crotonic acid, maleic anhydride and 2-acrylamido-2-methylpropanesulfonic acid as monomers. The acidic groups can be present in whole or in part as sodium, potassium, ammonium, mono- or triethanolammonium salt. Preferred monomers are 2-acrylamido-2-methylpropanesulfonic acid and acrylic acid. Very particularly preferred anionic polymers contain 2-acrylamido-2-methylpropanesulfonic acid as the sole monomer or as comonomer, it being possible for the sulfonic acid group to be wholly or partly in salt form. In this embodiment, it is preferred to use copolymers of at least one anionic monomer and at least one nonionic monomer. With regard to the anionic monomers, reference is made to the substances listed above. Preferred nonionic monomers are acrylamide, methacrylamide, acrylic acid ester, methacrylic acid ester, vinyl pyrrolidone, vinyl ether and vinyl ester. Preferred anionic copolymers are acrylic acid-acrylamide copolymers and in particular polyacrylamide copolymers with monomers containing sulfonic acid groups. A particularly preferred anionic copolymer consists of 70 to 55 mol% of acrylamide and 30 to 45 mol% of 2-acrylamido-2-methylpropanesulfonic acid, the sulfonic acid groups being wholly or partly as sodium, potassium, ammonium, mono- or triethanolammonium Salt. This copolymer can also be crosslinked, the crosslinking agents preferably being polyolefinic Unsaturated compounds such as tetraallyloxyethane, allyl sucrose, allylpentaerythritol and methylene bisacrylamide are used. Such a polymer is contained in the commercial product Sepigel ® 305 from SEPPIC. The use of this compound has proven to be particularly advantageous in the context of the teaching according to the invention. Also known as compound with isohexadecane and sold under the name Simulgel® ® 600 Polysorbate-80 sodium acryloyldimethyltaurate copoly- mers have proven effective as inventively particularly. Other particularly preferred anionic homopolymers and copolymers are uncrosslinked and crosslinked polyacrylic acids. Allyl ethers of pentaerythritol, sucrose and propylene can be preferred crosslinking agents. Such compounds are, for example, the commercial products Carbopol ® . A particularly preferred anionic copolymer contains 80-98% of an unsaturated, optionally substituted C 3 as monomer. 6- carboxylic acid or its anhydride and, if desired, 2 to 20% substituted acrylic acid esters of saturated C 1 -C 30 -carboxylic acids, it being possible for the copolymer to be crosslinked with the aforementioned crosslinking agents. Corresponding commercial products are Pemulen ® and the Carbopol ® types 954, 980, 1342 and ETD 2020 (ex BF Goodrich).
Geeignete nichtionische Polymere sind beispielsweise Polyvinylalkohole, die teilverseift sein können, z. B. die Handelsprodukte Mowiol® sowie Vinylpyrrolidon Vinylester-Copolymere und Polyvinylpyrrolidone, die z. B. unter dem Warenzeichen Luviskol® (BASF) vertrieben werden.Suitable nonionic polymers are, for example, polyvinyl alcohols, which can be partially saponified, e.g. B. the commercial products Mowiol ® and vinyl pyrrolidone vinyl ester copolymers and polyvinyl pyrrolidones, which, for. B. are sold under the trademark Luviskol ® (BASF).
Weitere Zusätze zu den kosmetisches oder pharmazeutisches Hautbehandlungsmitteln sind ausgewählt aus den Vitaminen, Provitaminen oder Vitaminvorstufen der Vitamin B-Gruppe oder deren Derivaten sowie den Derivaten von 2-Furanon. Zur Vitamin B-Gruppe oder zu dem Vitamin B-Komplex gehören unter anderemFurther additives to the cosmetic or pharmaceutical skin treatment agents are selected from the vitamins, provitamins or vitamin precursors of the vitamin B group or their derivatives and the derivatives of 2-furanone. The vitamin B group or the vitamin B complex include, among others
• Vitamin Bi, Trivialname Thiamin, chemische Bezeichung 3-[(4'-Amino-2'- methyl-5'-pyrimidinyl)-methyl]-5-(2-hydroxyethyl)-4-methylthiazoliumchlorid. Bevorzugt wird Thiaminhydrochlorid in Mengen von 0,05 bis 1 Gew.-%, bezogen auf das gesamte Mittel, eingesetzt.• Vitamin Bi, common name thiamine, chemical name 3 - [(4 ' -amino-2 ' - methyl-5 ' -pyrimidinyl) -methyl] -5- (2-hydroxyethyl) -4-methylthiazolium chloride. Thiamine hydrochloride is preferably used in amounts of 0.05 to 1% by weight, based on the total agent.
• Vitamin B2, Trivialname Riboflavin, chemische Bezeichung 7,8-Dimethyl-10- (1-D-ribityl)-benzo[g]pteridin-2,4(3/-/,10/-/)-dion. In freier Form kommt Riboflavin z. B. in Molke vor, andere Riboflavin-Derivate lassen sich aus Bakterien und Hefen isolieren. Ein erfindungsgemäß ebenfalls geeignetes Stereoisomeres des Riboflavin ist das aus Fischmehl oder Leber isolierbare Lyxoflavin, das statt des D-Ribityl einen D-Arabityl-Rest trägt. Bevorzugt werden Riboflavin oder seine Derivate in Mengen von 0,05 bis 1 Gew.-%, bezogen auf das gesamte Mittel, eingesetzt.• Vitamin B 2 , common name riboflavin, chemical name 7,8-dimethyl-10- (1-D-ribityl) -benzo [g] pteridine-2,4 (3 / - /, 10 / - /) - dione. In free form, riboflavin comes e.g. B. in whey before, other riboflavin derivatives can be isolated from bacteria and yeast. A stereoisomer of riboflavin which is also suitable according to the invention is lyxoflavin which can be isolated from fishmeal or liver and which carries a D-arabityl radical instead of D-ribityl. Riboflavin or its derivatives are preferably used in amounts of 0.05 to 1% by weight, based on the total agent.
• Vitamin B3. Unter dieser Bezeichnung werden häufig die Verbindungen Nicotinsäure und Nicotinsäureamid (Niacinamid) geführt. Erfindungsgemäß bevorzugt ist das Nicotinsäureamid, das in den erfindungsgemäßen kosmetischen und pharmazeutischen Zubereitungen bevorzugt in Mengen von 0,05 bis 1 Gew.-%, bezogen auf das gesamte Mittel, enthalten ist.• Vitamin B 3 . The compounds nicotinic acid and nicotinamide (niacinamide) are often listed under this name. The nicotinamide which is present in the cosmetic and pharmaceutical preparations according to the invention preferably in amounts of 0.05 to 1% by weight, based on the total composition, is preferred according to the invention.
• Vitamin B5 (Pantothensäure und Panthenol). Bevorzugt wird Panthenol eingesetzt. Erfindungsgemäß einsetzbare Derivate des Panthenols sind insbesondere die Ester und Ether des Panthenols sowie kationisch derivatisierte Panthenole. In einer weiteren bevorzugten Ausführungsform der Erfindung können an Stelle von sowie zusätzlich zu Pantothensäure oder Panthenol auch Derivate des 2-Furanon mit der allgemeinen Strukturformel (I) eingesetzt werden.• Vitamin B 5 (pantothenic acid and panthenol). Panthenol is preferably used. Derivatives of panthenol which can be used according to the invention are, in particular, the esters and ethers of panthenol and cationically derivatized panthenols. In a further preferred embodiment of the invention, instead of and in addition to pantothenic acid or panthenol, derivatives of 2-furanone with the general structural formula (I) can also be used.
Figure imgf000026_0001
(I)
Figure imgf000026_0001
(I)
Bevorzugt sind die 2-Furanon-Derivate, in denen die Substituenten R1 bis R6 unabhängig voneinander ein Wasserstoffatom, einen Hydroxylrest, einen Methyl-, Methoxy-, Aminomethyl- oder Hydroxymethylrest, einen gesättigten oder ein- oder zweifach ungesättigten, linearen oder verzweigten C2-C4 - Kohlenwasserstoffrest, einen gesättigten oder ein- oder zweifach ungesättigten, verzweigten oder linearen Mono-, Di- oder Trihydroxy-C2-C4 - Kohlenwasserstoffrest oder einen gesättigten oder ein- oder zweifach ungesättigten, verzweigten oder linearen Mono-, Di- oder Triamino-C2-C - Kohlenwasserstoffrest darstellen. Besonders bevorzugte Derivate sind die auch im Handel erhältlichen Substanzen Dihydro-3-hydroxy-4,4-dimethyl-2(3H)-furanon mit dem Trivialnamen Pantolacton (Merck), 4-Hydroxymethyl-γ-butyrolacton (Merck), 3,3-Dimethyl-2- hydroxy-γ-butyrolacton (Aldrich) und 2,5-Dihydro-5-methoxy-2-furanon (Merck), wobei ausdrücklich alle Stereoisomeren eingeschlossen sind. Das erfindungsgemäß außerordentlich bevorzugte 2-Furanon-Derivat ist Pantolacton (Dihydro-3- hydroxy-4,4-dimethyl-2(3H)-furanon), wobei in Formel (I) R1 für eine Hydroxylgruppe, R2 für ein Wasserstoff atom, R3 und R4 für eine Methylgruppe und R5 und R6 für ein Wasserstoffatom stehen. Das Stereoisomer (R)- Pantolacton entsteht beim Abbau von Pantothensäure.Preferred are the 2-furanone derivatives in which the substituents R 1 to R 6 independently of one another are a hydrogen atom, a hydroxyl radical, a methyl, methoxy, aminomethyl or hydroxymethyl radical, a saturated or mono- or di-unsaturated, linear or branched C 2 -C 4 - hydrocarbon radical, a saturated or mono- or di-unsaturated, represent branched or linear mono-, di- or trihydroxy-C 2 -C 4 - hydrocarbon residue or a saturated or mono- or di-unsaturated, branched or linear mono-, di- or triamino-C 2 -C 4 - hydrocarbon residue. Particularly preferred derivatives are the commercially available substances dihydro-3-hydroxy-4,4-dimethyl-2 (3H) -furanone with the common name pantolactone (Merck), 4-hydroxymethyl-γ-butyrolactone (Merck), 3.3 -Dimethyl-2-hydroxy-γ-butyrolactone (Aldrich) and 2,5-dihydro-5-methoxy-2-furanone (Merck), all stereoisomers being expressly included. The 2-furanone derivative which is extremely preferred according to the invention is pantolactone (dihydro-3-hydroxy-4,4-dimethyl-2 (3H) -furanone), wherein in formula (I) R 1 is a hydroxyl group, R 2 is a hydrogen atom , R 3 and R 4 represent a methyl group and R 5 and R 6 represent a hydrogen atom. The stereoisomer (R) - pantolactone is formed when pantothenic acid is broken down.
Die genannten Verbindungen des Vitamin B5-Typs sowie die 2-Furanonderivate sind in den erfindungsgemäßen kosmetischen und pharmazeutischen Zubereitungen bevorzugt in einer Gesamtmenge von 0,05 bis 10 Gew.-%, bezogen auf das gesamte Mittel, enthalten. Gesamtmengen von 0,1 bis 5 Gew.-% sind besonders bevorzugt.The above-mentioned compounds of the vitamin B 5 type and the 2-furanone derivatives are preferably present in the cosmetic and pharmaceutical preparations according to the invention in a total amount of 0.05 to 10% by weight, based on the total composition. Total amounts of 0.1 to 5% by weight are particularly preferred.
• Vitamin Bβ, wobei man hierunter keine einheitliche Substanz, sondern die unter den Trivialnamen Pyridoxin, Pyridoxamin und Pyridoxal bekannten Derivate des 5-Hydroxymethyl-2-methylpyhdin-3-ols versteht. Vitamin B6 ist in den erfindungsgemäßen kosmetischen und pharmazeutischen Zubereitungen bevorzugt in Mengen von 0,0001 bis 1 ,0 Gew.-%, insbesondere in Mengen von 0,001 bis 0,01 Gew.-%, enthalten.• Vitamin Bβ, which does not mean a uniform substance, but rather the derivatives of 5-hydroxymethyl-2-methylpyhdin-3-ol known under the common names pyridoxine, pyridoxamine and pyridoxal. Vitamin B 6 is contained in the cosmetic and pharmaceutical preparations according to the invention preferably in amounts of 0.0001 to 1.0% by weight, in particular in amounts of 0.001 to 0.01% by weight.
• Vitamin B7 (Biotin), auch als Vitamin H oder "Hautvitamin" bezeichnet. Bei Biotin handelt es sich um (3aS,4S,6aR)-2-Oxohexahydrothienol[3,4- ]-imidazol-4- valeriansäure. Biotin ist in den erfindungsgemäßen kosmetischen und pharmazeutischen Zubereitungen bevorzugt in Mengen von 0,0001 bis 1 ,0 Gew.- %, insbesondere in Mengen von 0,001 bis 0,01 Gew.-% enthalten. Panthenol, Pantolacton, Nicotinsäureamid sowie Biotin sind erfindungsgemäß ganz besonders bevorzugt.• Vitamin B 7 (biotin), also known as vitamin H or "skin vitamin". Biotin is (3aS, 4S, 6aR) -2-oxohexahydrothienol [3,4-] imidazole-4-valeric acid. The cosmetic and pharmaceutical preparations according to the invention preferably contain biotin in amounts of 0.0001 to 1.0% by weight, in particular in amounts of 0.001 to 0.01% by weight. Panthenol, pantolactone, nicotinamide and biotin are very particularly preferred according to the invention.
Die erfindungsgemäß verwendeten kosmetischen Zubereitungen eignen sich bevorzugt zur kosmetischen Behandlung der Cellulite und von lokalen Fettübergewichten, aber auch zur Verwendung in sogenannten "Slimming- Produkten" und zur Straffung der Haut, insbesondere der Haut von Beinen, Dekollete, Hals oder im Gesichtsbereich.The cosmetic preparations used according to the invention are preferably suitable for the cosmetic treatment of cellulite and local excess fat, but also for use in so-called "slimming products" and for tightening the skin, in particular the skin of legs, décolleté, neck or in the facial area.
Ein weiterer Gegenstand der Erfindung ist die Verwendung einer Zusammensetzung, umfassend ein Flavon, Isoflavon oder deren Glykosid und gegebenenfalls einen Stoff, der C-Nervenfasern stimuliert und/oder depolarisiert, zur Herstellung einer Zubereitung zur therapeutischen Behandlung der Cellulite.Another object of the invention is the use of a composition comprising a flavone, isoflavone or their glycoside and optionally a substance which stimulates and / or depolarizes C-nerve fibers for the production of a preparation for the therapeutic treatment of cellulite.
Zur Herstellung pharmazeutischer Zubereitungen lassen sich die Wirkstoffe der drei vorstehend genannten Gruppen, gegebenenfalls in Kombination mit anderen Wirksubstanzen, zusammen mit einem oder mehreren inerten üblichen Trägerstoffen und/oder Verdünnungsmitteln, z. B. mit Maisstärke, Milchzucker, Rohrzucker, Sorbitol, mikrokristalliner Cellulose, Magnesiumstearat, Polyvinylpyrrolidon, Zitronensäure, Weinsäure, Wasser, Wasser/Ethanol, Wasser/Glycerin, Wasser/Sorbit, Wasser/Polyethylenglykol, Propylenglykol, Carboxymethylcellulose oder fetthaltigen Substanzen wie Hartfett oder deren geeigneten Gemischen, in übliche galenische Zubereitungen wie Tabletten, Dragees, Kapseln, Pulver, Suspensionen, Tropfen, Ampullen, Säfte oder Zäpfchen einarbeiten. Die zur Erzielung einer entsprechenden Wirkung bei pharmazeutischen Anwendungen erforderliche tägliche Dosierung des Wirkstoffs oder Wirkstoffgemischs beträgt zweckmäßigerweise 0,1 bis 10 mg/kg Körpergewicht, vorzugsweise 0,5 bis 2 mg/kg Körpergewicht .For the preparation of pharmaceutical preparations, the active ingredients of the three groups mentioned above, optionally in combination with other active substances, together with one or more inert customary carriers and / or diluents, for. B. with corn starch, milk sugar, cane sugar, sorbitol, microcrystalline cellulose, magnesium stearate, polyvinylpyrrolidone, citric acid, tartaric acid, water, water / ethanol, water / glycerol, water / sorbitol, water / polyethylene glycol, propylene glycol, carboxymethyl cellulose or fatty substances such as hard fat or the like suitable mixtures, work into conventional galenical preparations such as tablets, dragees, capsules, powders, suspensions, drops, ampoules, juices or suppositories. The daily dosage of the active ingredient or mixture of active ingredients required to achieve a corresponding effect in pharmaceutical applications is advantageously 0.1 to 10 mg / kg body weight, preferably 0.5 to 2 mg / kg body weight.
Die erfindungsgemäßen pharmazeutischen Zubereitungen eignen sich vorzugsweise zur therapeutischen Behandlung der Cellulite. Die Herstellung der erfindungsgemäßen Zusammensetzungen erfolgt dadurch, dass die wässrige Phase, die wasserlösliche Wirk- und Inhaltsstoffe sowie gegebenenfalls wasserlösliche Emulgatoren enthält, und die Ölphase, die Fette, Öle, öllösliche Wirkstoffe und gegebenenfalls öllösliche Emulgatoren enthält, bei einer Temperatur von 10 bis 90 °C intensiv miteinander vermischt werden.The pharmaceutical preparations according to the invention are preferably suitable for the therapeutic treatment of cellulite. The compositions according to the invention are prepared in that the aqueous phase, which contains water-soluble active ingredients and ingredients and, if appropriate, water-soluble emulsifiers, and the oil phase which contains fats, oils, oil-soluble active ingredients and optionally oil-soluble emulsifiers, at a temperature of 10 to 90 ° C are mixed intensively.
Die folgenden Beispiele sollen die vorliegende Erfindung verdeutlichen. Alle Prozentanteile sind, soweit nicht anders angegeben, auf das Gesamtgewicht der Zubereitungen bezogen. The following examples are intended to illustrate the present invention. Unless otherwise stated, all percentages are based on the total weight of the preparations.
Beispiele:Examples:
Beispiel 1 : RezepturenExample 1: Recipes
Anti-Cellulite-GeleAnti-cellulite gels
Figure imgf000030_0001
Figure imgf000030_0001
Anti-Cellulite-CremesAnti-cellulite creams
Figure imgf000031_0001
Figure imgf000031_0001
Anti-Cellulite-LotionenAnti-cellulite lotions
Figure imgf000032_0001
Figure imgf000032_0001
Beispiel 2: TestergebnisseExample 2: Test results
In einem vierwöchigen Gebrauchstest wurde das Anti-Cellulite-Gel nach Beispiel 1 mit der Rezeptur Gel-5 auf seine Wirksamkeit in Bezug auf das Cellulite-Phänomen und seine kosmetische Akzeptanz bei 25 Frauen getestet (Halbseitentest gegen Placebo). Die Testteilnehmerinnen wurden direkt nach dem Gebrauchstest zur Wirksamkeit des Produktes und der kosmetischen Akzeptanz in standardisierter Weise befragt.In a four-week use test, the anti-cellulite gel according to Example 1 with the formulation Gel-5 was tested for its effectiveness in relation to the cellulite phenomenon and its cosmetic acceptance in 25 women (half-side test against placebo). The test participants were asked directly after the use test about the effectiveness of the product and the cosmetic acceptance in a standardized way.
Über 80% der Probandinnen spürten ein prickelndes und erwärmendes Hautgefühl. Schon nach vierwöchiger Anwendung konnten 28% der Frauen eine Verbesserung der Cellulite-Symptomatik feststellen und 40% der Frauen verzeichneten eine Verbesserung der Hautfestigkeit. 84% waren mit der Hautverträglichkeit des Produktes zufrieden und 72% konnten sich vorstellen, das Produkt weiter zu verwenden. Over 80% of the test subjects felt a tingling and warming skin feeling. After only four weeks of use, 28% of women noticed an improvement in cellulite symptoms and 40% of women reported an improvement in skin firmness. 84% were satisfied with the skin tolerance of the product and 72% could imagine using the product again.

Claims

Patentansprüche: claims:
1. Verwendung einer Zusammensetzung, umfassend ein Flavon, Isoflavon oder deren Glykosid und gegebenenfalls einen Stoff, welcher C-Nervenfasern stimuliert und/oder depolarisiert, zur kosmetischen Behandlung von Cellulite oder zur Straffung der Haut.1. Use of a composition comprising a flavone, isoflavone or their glycoside and optionally a substance which stimulates and / or depolarizes carbon nerve fibers, for the cosmetic treatment of cellulite or for firming the skin.
2. Verwendung einer Zusammensetzung, umfassend ein Flavon, Isoflavon oder deren Glykosid und gegebenenfalls einen Stoff, welcher C-Nervenfasern stimuliert und/oder depolarisiert, zur Herstellung einer pharmazeutischen Zubereitung zur therapeutischen Behandlung von Cellulite.2. Use of a composition comprising a flavone, isoflavone or their glycoside and optionally a substance which stimulates and / or depolarizes C-nerve fibers for the production of a pharmaceutical preparation for the therapeutic treatment of cellulite.
3. Verwendung nach einem der Ansprüche 1 oder 2, dadurch gekennzeichnet, dass das Flavon, Isoflavon oder deren Glykosid Bestandteil eines aus einer Pflanze gewonnenen Substanzgemisches ist.3. Use according to one of claims 1 or 2, characterized in that the flavone, isoflavone or their glycoside is part of a mixture of substances obtained from a plant.
4. Verwendung nach Anspruch 3, dadurch gekennzeichnet, dass das Substanzgemisch aus Soja gewonnen wird.4. Use according to claim 3, characterized in that the substance mixture is obtained from soy.
5. Verwendung nach einem der Ansprüche 1 bis 4, dadurch gekennzeichnet, dass das Flavon oder Flavonglykosid ausgewählt ist aus der Gruppe, die gebildet wird von Quercetin, Rutin, Hesperidin und deren Gemischen.5. Use according to one of claims 1 to 4, characterized in that the flavone or flavone glycoside is selected from the group formed by quercetin, rutin, hesperidin and mixtures thereof.
6. Verwendung nach einem der Ansprüche 1 bis 4, dadurch gekennzeichnet, dass das Isoflavon oder Isoflavonglykosid ausgewählt ist aus der Gruppe, die gebildet wird von Daidzein, Genistein, Glycitein, Formononetin, Daidzin, Genistin und deren Gemischen.6. Use according to one of claims 1 to 4, characterized in that the isoflavone or isoflavone glycoside is selected from the group formed by daidzein, genistein, glycitein, formononetin, daidzin, genistin and mixtures thereof.
7. Verwendung nach Anspruch 1 oder 2, dadurch gekennzeichnet, dass der die C- Nervenfasem stimulierende Stoff ausgewählt ist aus der Gruppe, die gebildet wird von Capsaicin, N-Vanillyl-nonanamid, deren Glykosiden und Gemischen der vorstehenden Substanzen. 7. Use according to claim 1 or 2, characterized in that the C-nerve fiber stimulating substance is selected from the group formed by capsaicin, N-vanillyl-nonanamide, their glycosides and mixtures of the above substances.
8. Verwendung nach einem der Ansprüche 1 bis 7, dadurch gekennzeichnet, dass die Zubereitung zusätzlich einen Phosphodiesterase-Inhibitor enthält.8. Use according to one of claims 1 to 7, characterized in that the preparation additionally contains a phosphodiesterase inhibitor.
9. Verwendung nach Anspruch 8, dadurch gekennzeichnet, dass der Phosphodiesterase-Inhibitor ausgewählt ist aus Xanthin und Methylxanthin.9. Use according to claim 8, characterized in that the phosphodiesterase inhibitor is selected from xanthine and methylxanthine.
10. Verwendung nach einem der Ansprüche 1 bis 9, dadurch gekennzeichnet, dass die Zubereitung insgesamt 0,1 bis 20 Gew.-% an einem oder mehreren Flavonen, Isoflavonen oder deren Glykosiden, jeweils bezogen auf das Gesamtgewicht der Zubereitung, enthält.10. Use according to one of claims 1 to 9, characterized in that the preparation contains a total of 0.1 to 20 wt .-% of one or more flavones, isoflavones or their glycosides, each based on the total weight of the preparation.
11.Verwendung nach einem der Ansprüche 1 bis 9, dadurch gekennzeichnet, dass die Zubereitung insgesamt 1 bis 10 Gew.-% an einem oder mehreren Flavonen, Isoflavonen oder deren Glykosiden, jeweils bezogen auf das Gesamtgewicht der Zubereitung, enthält.11.Use according to one of claims 1 to 9, characterized in that the preparation contains a total of 1 to 10 wt .-% of one or more flavones, isoflavones or their glycosides, each based on the total weight of the preparation.
12. Verwendung nach einem der Ansprüche 1 bis 9, dadurch gekennzeichnet, dass die Zubereitung insgesamt 0,0001 bis 3 Gew.-% an einem oder mehreren Stoffen enthält, welche die C-Nervenfasern der Haut stimulieren und/oder depolarisieren, jeweils bezogen auf das Gesamtgewicht der Zubereitung.12. Use according to one of claims 1 to 9, characterized in that the preparation contains a total of 0.0001 to 3 wt .-% of one or more substances which stimulate and / or depolarize the C-nerve fibers of the skin, in each case based on the total weight of the preparation.
13. Verwendung nach einem der Ansprüche 1 bis 9, dadurch gekennzeichnet, dass die Zubereitung insgesamt 0,005 bis 0,5 Gew.-% an einem oder mehreren Stoffen enthält, welche die C-Nervenfasern der Haut stimulieren und/oder depolarisieren, jeweils bezogen auf das Gesamtgewicht der Zubereitung.13. Use according to one of claims 1 to 9, characterized in that the preparation contains a total of 0.005 to 0.5% by weight of one or more substances which stimulate and / or depolarize the C-nerve fibers of the skin, in each case based on the total weight of the preparation.
14. Verwendung nach einem der Ansprüche 8 oder 9, dadurch gekennzeichnet, dass die Zubereitung insgesamt 1 bis 15 Gew.-% und vorzugsweise 5 bis 10 Gew.-% an einem oder mehreren Phosphodiesterase-inhibitoren, jeweils bezogen auf das Gesamtgewicht der Zubereitung, enthält. 14. Use according to one of claims 8 or 9, characterized in that the preparation in total 1 to 15 wt .-% and preferably 5 to 10 wt .-% of one or more phosphodiesterase inhibitors, each based on the total weight of the preparation, contains.
15. Verwendungen nach einem der Ansprüche 1 bis 14, dadurch gekennzeichnet, dass die Zubereitungen ein oder mehrere übliche kosmetische und/oder pharmazeutische Hilfsstoffen umfasst, welche ausgewählt sind aus Fetten, Ölen, Wachsen, Silikonen, Emulgatoren, Antioxidantien, Vitaminen, Lichtschutzfiltern, Mono-, Oligo- und Polysacchariden, Duftstoffen, Farbstoffen, Verdickungsmitteln, anfeuchtenden und/oder feuchthaltenden Substanzen, Tensiden, Pflanzenextrakten, Aromen, weiteren Süßungsmitteln, Adsorbentien und weitere Wirk- und Hilfsstoffen15. Uses according to one of claims 1 to 14, characterized in that the preparations comprise one or more customary cosmetic and / or pharmaceutical auxiliaries which are selected from fats, oils, waxes, silicones, emulsifiers, antioxidants, vitamins, light protection filters, mono -, Oligo- and polysaccharides, fragrances, dyes, thickeners, moisturizing and / or moisturizing substances, surfactants, plant extracts, aromas, other sweeteners, adsorbents and other active substances and auxiliary substances
16. Verwendung nach einem der Ansprüche 1 bis 15, dass die Zubereitung eine Substanz, ausgewählt aus den Vitaminen, Provitaminen oder Vitaminvorstufen der Vitamin B-Gruppe oder deren Derivaten sowie den Derivaten von 2-Furanon enthält.16. Use according to one of claims 1 to 15, that the preparation contains a substance selected from the vitamins, provitamins or vitamin precursors of the vitamin B group or their derivatives and the derivatives of 2-furanone.
17. Verwendung nach einem der Ansprüche 1 bis 16, dadurch gekennzeichnet, dass die Zubereitung ein oder mehrere filmbildende, emulsionsstabilisierende, verdickende oder adhäsive Polymere, ausgewählt aus natürlichen und synthetischen Polymeren, die kationisch, anionisch, amphoter geladen oder nichtionisch sein können, enthalten.17. Use according to one of claims 1 to 16, characterized in that the preparation contains one or more film-forming, emulsion-stabilizing, thickening or adhesive polymers, selected from natural and synthetic polymers, which can be cationic, anionic, amphoteric or non-ionic.
18. Verwendung nach einem der Ansprüche 1 bis 17, dadurch gekennzeichnet, dass die kosmetische oder pharmazeutische Zubereitung in Form eines Öls, einer Salbe, eines Gels oder in Form einer creme- oder milchartigen Öl-in-Wasser- oder Wasser-in-ÖI-Emulsion vorliegt.18. Use according to one of claims 1 to 17, characterized in that the cosmetic or pharmaceutical preparation in the form of an oil, an ointment, a gel or in the form of a creamy or milky oil-in-water or water-in-oil Emulsion is present.
19. Verfahren zur Herstellung einer gemäß den Ansprüchen 1 bis 18 verwendeten Zusammensetzung, dadurch gekennzeichnet, dass die wässrige Phase und die Ölphase bei einer Temperatur von 10 bis 90 °C intensiv miteinander vermischt werden. 19. A method for producing a composition used according to claims 1 to 18, characterized in that the aqueous phase and the oil phase are mixed intensively with one another at a temperature of 10 to 90 ° C.
PCT/EP2001/002070 2000-02-28 2001-02-23 Use of flavones or isoflavones for the treatment of cellulite WO2001064177A1 (en)

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DE10009424A DE10009424A1 (en) 2000-02-28 2000-02-28 Use of flavone and isoflavone compounds, especially of plant origin, for the treatment of cellulite
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US6617349B2 (en) 2000-08-16 2003-09-09 Lipton, Division Of Conopco, Inc. Blends of isoflavones and flavones
DE10218476A1 (en) * 2002-04-25 2003-11-06 Beiersdorf Ag Medicaments, cosmetics and dermatological compositions for a wide variety of skin treatments contain lignans or their glycosides
FR2841470A1 (en) * 2002-06-27 2004-01-02 Pharmascience Lab USE OF ISOFLAVONES FOR THE PREPARATION OF TOPICAL COMPOSITIONS USEFUL FOR PROMOTING SLIMMING AND ASSOCIATED COSMETIC TREATMENT METHOD
WO2004064712A2 (en) * 2003-01-17 2004-08-05 Beiersdorf Ag Preparations containing bean sprout extracts combined with vitamin c and/or e and/or $g(a)-glycosylrutin
EP1541127A1 (en) * 2003-12-10 2005-06-15 L'oreal Use of modulators of aquaglyceroporins as slimming agents
FR2868701A1 (en) * 2004-04-07 2005-10-14 Provital S A Sa Composition for controlling fat content and differentiation of adipocytes, useful for treating cellulite, comprising dihydroflavonol, e.g. dihydromyricetin
JP2006527725A (en) * 2003-06-17 2006-12-07 ディーエスエム アイピー アセッツ ビー.ブイ. Topical drugs containing phytanic acid or its derivatives
FR2919501A1 (en) * 2007-08-02 2009-02-06 Oreal USE OF HESPERIDINE OR ONE OF ITS DERIVATIVES FOR THE PREVENTION AND / OR TREATMENT OF RELEASED SKIN
WO2014091147A2 (en) 2012-12-11 2014-06-19 Isp Investments Inc. Cosmetic use of the combination of a carob germ extract and caffeine as a slimming active agent
WO2014091146A2 (en) 2012-12-11 2014-06-19 Isp Investments Inc. Cosmetic use of a carob seed extract as a slimming active agent
WO2018048892A1 (en) 2016-09-07 2018-03-15 Isp Investments Llc Method for increasing lipolysis using a composition comprising bioactive nelumbo nucifera (lotus) extract
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US6617349B2 (en) 2000-08-16 2003-09-09 Lipton, Division Of Conopco, Inc. Blends of isoflavones and flavones
EP1180331A1 (en) * 2000-08-16 2002-02-20 Unilever N.V. Blends of isoflavones and flavones
DE10218476A1 (en) * 2002-04-25 2003-11-06 Beiersdorf Ag Medicaments, cosmetics and dermatological compositions for a wide variety of skin treatments contain lignans or their glycosides
FR2841470A1 (en) * 2002-06-27 2004-01-02 Pharmascience Lab USE OF ISOFLAVONES FOR THE PREPARATION OF TOPICAL COMPOSITIONS USEFUL FOR PROMOTING SLIMMING AND ASSOCIATED COSMETIC TREATMENT METHOD
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WO2004064712A2 (en) * 2003-01-17 2004-08-05 Beiersdorf Ag Preparations containing bean sprout extracts combined with vitamin c and/or e and/or $g(a)-glycosylrutin
WO2004064712A3 (en) * 2003-01-17 2005-03-03 Beiersdorf Ag Preparations containing bean sprout extracts combined with vitamin c and/or e and/or $g(a)-glycosylrutin
JP2006527725A (en) * 2003-06-17 2006-12-07 ディーエスエム アイピー アセッツ ビー.ブイ. Topical drugs containing phytanic acid or its derivatives
EP1541127A1 (en) * 2003-12-10 2005-06-15 L'oreal Use of modulators of aquaglyceroporins as slimming agents
FR2863492A1 (en) * 2003-12-10 2005-06-17 Oreal USE OF AQUAGLYCEROPORIN MODULATORS AS SLIMMING
FR2868701A1 (en) * 2004-04-07 2005-10-14 Provital S A Sa Composition for controlling fat content and differentiation of adipocytes, useful for treating cellulite, comprising dihydroflavonol, e.g. dihydromyricetin
FR2919501A1 (en) * 2007-08-02 2009-02-06 Oreal USE OF HESPERIDINE OR ONE OF ITS DERIVATIVES FOR THE PREVENTION AND / OR TREATMENT OF RELEASED SKIN
WO2009022077A3 (en) * 2007-08-02 2010-02-11 L'oreal Use of hesperidin or of a derivative thereof for the prevention and/or treatment of slackened skin
WO2014091147A2 (en) 2012-12-11 2014-06-19 Isp Investments Inc. Cosmetic use of the combination of a carob germ extract and caffeine as a slimming active agent
WO2014091146A2 (en) 2012-12-11 2014-06-19 Isp Investments Inc. Cosmetic use of a carob seed extract as a slimming active agent
US9962329B2 (en) 2012-12-11 2018-05-08 ISP Investments, LLC Cosmetic use of the combination of a carob germ extract and caffeine as a slimming active agent
WO2018048892A1 (en) 2016-09-07 2018-03-15 Isp Investments Llc Method for increasing lipolysis using a composition comprising bioactive nelumbo nucifera (lotus) extract
EP3970691A1 (en) 2020-09-18 2022-03-23 C.F.E.B. Sisley Slimming cosmetic compositions containing one or more limonoids
FR3114241A1 (en) 2020-09-18 2022-03-25 C F E B Sisley Slimming cosmetic compositions containing one or more limonoids

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