WO2003079963A2

WO2003079963A2 - Homeopathic modular complex

Info

Publication number: WO2003079963A2
Application number: PCT/FR2003/000901
Authority: WO
Inventors: Pierre Wunsch
Original assignee: Pierre Wunsch
Priority date: 2002-03-22
Filing date: 2003-03-20
Publication date: 2003-10-02
Also published as: AU2003233390A1; FR2837381A1; WO2003079963A3; AU2003233390A8

Abstract

The invention concerns a phyto-homeopathic modular complex for dermatological use comprising a plurality of dyes. Said plurality of dyes includes at least a Santalinus parent dye and a Sassafras officinalis parent dye, and a carrier. In a preferred embodiment, said complex comprises about 20 % of each of the two said parent dyes, about 50 % of a carrier, the rest consisting of other adjuvant dyes. The invention is in particular applicable to hair growth.

Description

Modular Phyto-Homeopathic Complex

TECHNICAL FIELD OF THE INVENTION

The lotion that we are experimenting with is an entirely natural product, a complex of homeopathic mother tinctures (T.M.), devoid of any toxicity. It has a regulating action on the sebaceous secretion of the scalp, an anti-fall action which manifests itself from the first applications and above all a spectacular effect with the appearance of young hair on very advanced alopecia which can be classified in stage 3 d 'after HAMILTON. The alopecia concerned is androgenetic and excludes any underlying pathology, similarly it concerns only male subjects.

This discovery, to benefit from a scientific basis capable of accrediting it, obliges to expose the physiology of the pilosebaceous follicle and its close hormonal interdependence.

THE PILO-SEBACE FOLLICLE

As the name suggests, the pilosebaceous follicle brings together the systematic association of 2 tissues: the hair follicle and the sebaceous gland; in humans, the pilosebaceous follicle presents an extreme diversity according to the cutaneous sites. According to the respective size of these 2 entities, there are 3 main types: the terminal pilosebaceous follicles where the hair follicle takes its most intense development associated with sebaceous glands of relatively small dimension. This is the typical case encountered in the scalp, cheeks and, in men, the beard or armpits.

The pilosebaceous follicles known as sebaceous follicles or, conversely, the hair follicle is reduced to 1 'state of down associated with very developed sebaceous glands ultilobe (forehead, nose wings, chin).

The pilosebaceous follicles or the 2 tissues are of weak development, it is the case of the regions of the members producing wispy hairs and a very weak sebaceous excretion.

The existence of a follicular canal is the characteristic common to all three types. Its dimension is very variable according to the types with a diameter varying from 10 to 120 microns and a depth from 0.4 to 4 mm.

The density of the pilosebaceous follicles is very variable ranging from 200 to 300 / cm ² (scalp, forehead) to 10-20 / cm ² on the forearm.

A point to emphasize here is the distinction of the human hair follicle from that of other animal species. In humans, it produces 2 types of anatomical fibers of identical elementary composition but whose synthesis responds to different physiological stimuli: - the hair appears during the pubertal period (beard, armpits, pubic hair), under androgenic stimulation. Hair growth does not respond to these criteria since it is present and grows in the pubescent child.

The growth of the hair is not regular throughout life unlike the hair. The most obvious example is the elderly alopecics with the beard provided. Hair growth proceeds in successive cycles:

The so-called anagen growth phase with an average duration of 3 years (ranging from 2 to 8 years) where the growth speed is considered to be constant.

The so-called catagen rest phase lasting 3 weeks or the initial bulb keratinizes and rises to the surface of the skin.

Finally, a last important point that characterizes the human species is that each hair follicle, among the 100,000 to 120,000 that has a hair has its own cycle and completely independent of its neighbor.

THE SEBACEOUS GLAND. Annexed to the hairs and the hair, its main role is to secrete sebum, as we have seen previously, its size and density of distribution vary depending on the location. The sebaceous secretion takes place in three stages: the production of sebum at the level of the gland, its transfer in the follicular canal, its excretion on the surface of the epidermis.

Like the hair follicle, its functioning is strongly influenced by androgens: eunuchs and castrates secrete less sebum (50%) than control groups, in different animal experiments such as the flank organ of the hamster and the preputial gland of the rat, castration has been shown to cause atrophy of these glands, atrophy which will be restored by the administration of androgens.

METABOLISM OF ANDROGENS. Androgens are steroid hormones, that is, they are produced from cholesterol.

SUMMARY: Schematically, circulating androgens come from the secretion of adrenals and testes in humans; in women 50% of the adrenals, ovaries; and 50% of a peripheral inter-conversion.

TRANSPORT: In the blood, these hormones circulate largely linked to plasma proteins mainly to SHBG (sex hormone binding globulin). The free fraction is relatively small, it represents the biologically active fraction because it alone can cross the cell barrier of the target organ to exert its action, as is the case with testosterone.

PERIPHERAL METABOLISM: These androgens, in their native state, cannot maintain the secondary sexual characteristics, a part which escapes the hepatic metabolism penetrates the skin, it is the key stage of their transformation into biologically active hormones. The skin has the dual characteristic of being both the site of androgen metabolism and the target organ of androgens that it receives or produces. In the case which interests us, free testosterone penetrates the skin and undergoes at the level of the pilosebaceous follicle a reduction which transforms it into dihydrotestosterone (DHT) thanks to the presence at the level of the pilosebaceous follicle, of an enzyme: 5alpha reductase. DHT represents the active form of the hormone. This capacity, more important of in situ transformation of weak androgens into potent androgens could be a critical point in the pathogenesis of androgenic alopecia. In the target cell, DHT then combines with a high-affinity membrane receptor which leads it to the nucleus. The DHT receptor complex then interacts with another specific protein, the nuclear acceptor. The new complex thus formed transmits information to the cell which will activate the biological effects: synthesis of sebum, hair growth.

At this stage, it should be pointed out that 5alpha-reductase is also present in the pilosebaceous follicle of beard hair, armpits, pubic hair, and that the effect of androgens, in particular testosterone, differs and even opposes depending on the skin site: stimulation of beard growth, no effect on the eyelashes, involution on the scalp. Thus the differences in hair growth observed in the same subject, both alopecic and with a well-supplied beard, are due to genetic differences in the hair follicles themselves, depending on the skin territory, because the dosage of testosterone level in the alopecic subject is normal.

Ultimately, the initial disorder in the genesis of alopecia seems to be on several levels: a. A transport anomaly due to a deficit in the concentration of SHBG (sex hormone binding globulin), this is confirmed by the plasma assays carried out in male androgenic alopecia with a lower level of SHBG and high levels of free testosterone measured in saliva. So super physiological levels of this hormone would penetrate the target organ explaining the deleterious effect. b. An alteration of the mechanism initiating the biological effect in the nucleus of the cell, when the hormone-acceptor nuclear complex enters it to express the hormonal message. vs. An hyperactivity of 5alpha reductase in the skin of the alopecic which is confirmed by sophisticated assays currently in the field of research. But the disorder here can be primary related to a structural anomaly of the enzyme or secondary to the hormonal hyper stimulation taking into account what precedes.

STATE OF THE PRIOR ART. The treatments currently available in androgenic alopecia are numerous, medical and cosmetological.

Medical treatments Conventional medical treatment is based on the combination of vitamin B5 (Bepanthene) and vitamin H or B8 (Biotin). This therapy has remained ineffective, at most it can slow the fall at the cost of continuous treatment, but in no case does it avoid the progression to alopecia.

Amino acids are used for their antiseborrheic and antioxidant anti-aging action on the connective tissue. The result is equivalent to the previous therapy, these are Cystine, la- Lobamine-Cysteine. Gelucystine: vitamin B6 also has an anti-seborrheic role by inhibition of 5alpha-reductase and perhaps, for direct contribution of a trace element which makes part of the synthesis of hair keratin. The treatment is done at the rate of 2 to 6 capsules per day (Rubizinc). The effectiveness on hair regrowth is disappointing. Minoxidil, the action of which was discovered fortuitously by the use of Lonoten "per os" as an antihypertensive, has confirmed an anti-fall action in 30 to 40% of cases of male androgenic alopecia. The long-term effects, despite regular application, remain modest: in fact, a down appears, which then weakens and disappears over time.

Finasteride: starting from the observation of a more intense activity of 5alpha reductase in bald people, the idea of using Finasteride in this indication made sense. Indeed, this drug has been a 5alphareductase inhibitor for several years in benign prostatic hypertriophy (prostate adenoma) at a dose of 5 mg per day. The studies published in the literature have demonstrated, first of all, that it is more effective than placebo, which should be emphasized because, in the treatment of all forms of confirmed alopecia, this fact had only been demonstrated before with Minoxidil for local use which we will discuss below. Studies on Finasteride at 1 mg per day have also shown after one year of daily treatment, regrowth of the order of 10% on the vertex in mild to moderate alopecia (2 to 5 of the Hamilton classification). On the other hand, the regrowth increases only very slightly during the second year of treatment. The overall regrowth induced by Finasteride is therefore only modest and, in our opinion, Finasteride should rather used as a fall arrester, as a brake on the evolution of androgenetic alopecia.

Anti-androgen treatments are general (Cyproterone) or local (Progestosel, Delipoderm). Cyproterone (androcur and Diane 35) has obviously modified the evolution of female androgenic alopecia and suppressed the alopecia of the pills with norsteroids, unfortunately, it is not usable in men because of the risk of feminization (drug castration ). Progestosol is a weakly active 5alpha reductase antagonist. Delipoderm is an estrogen with little effectiveness on the scalp.

Dermo-cosmetological treatments exist in a large number of preparations for the general public, either 'per os' or locally. Among the preparations & 'per os' include Nutricap, Forcapil, Forvital, Phyto vitamin. For local use, we can mention Foltène Forcapil, Fabrame, Bioscalin. Here too, the results remain disappointing.

Surgery

Surgical treatments for diffuse alopecia are rarely possible, except when there is a limited alopecic area and a sufficiently dense occipital donor area.

Results with the application of the new lotion

The new hair lotion consists of an excipient, a group of six stimulants, Mother Tinctures of homeopathic phytotherapy, two of which are natural dyes, and a plant oil. The excipient can be physiological serum, a pure phytotherapeuthic oil or a commercial hair lotion: its ratio will be 50%.

The physiological stimulants are: 1) SANTALINUS, Homeopathic Mother Tincture, and 2) SASSAFRAS OFFICINAL, Homeopathic Mother Tincture. The ratio will be 20% for each of them. These two mother tinctures are the key components of the complex. They are the ones that bring hair roots back to life by reactivating the hair regrowth mechanism and regenerating the scalp, giving it suppleness and vitality.

But it is SANTALINUS T.M. that has the greatest stimulating power. It is capable, on its own, of restoring texture and vigor to hair, of stimulating hair growth, or even of initiating the regrowth mechanism.

They are also the ones which contain the natural dyes fulfilling two functions: the first being to color, for 24 hours, gray or white hair in a reddish color. The second is, it seems to us, to stimulate the production of melanin (regenerative function), thus gradually restoring their natural color to the hair (around three to six months for regrowth). Homeopathic growth adjuvants:

- ROSMARINUS OFFICINALIS, Homeopathic Mother Tincture. The ratio will be 5%. The mother tincture of Rosmarinus is also a stimulant that awakens atonies. It is here, in the complex, an excellent adjuvant for cellular revitalization. - ARCTIUM LAPPA, Homeopathic Mother Tincture. The ratio will be 5%. This mother tincture is known to promote hair growth.

Blood circulation stimulants: CUPRESSUS SEMPERVIRENS, Homeopathic Mother Tincture; GINKGO BILOBA, Homeopathic Mother Tincture. The ratio will be 250 drops, for 250 ml. They have the function of activating the blood circulation to supply the scalp and the hair roots. They also help in better penetration of the revitalizing elements of the complex into the cells of the dermis.

The phytotherapeuthic growth adjuvant: CAMELIA JAPONICA oil. The ratio will be 250 drops for 250 ml. This natural and pure oil allows the lotion to adhere better to the hair, preventing it from drying out, while nourishing young hair with its vitamin E. It also attenuates, by darkening, the lively tone of the coloring dyes.

However, it seems obvious that the amazing effectiveness of this complex comes from the synergy of its components and its remarkably balanced composition (this formula is specific to hair lotion).

The treatment of alopecia consisted of the application of the lotion at the frequency of 2 times per day, followed by a moderate massage of the scalp by privileging the most alopecic zones. In our test, alopecia reaches stage 3 according to the classification of HAMILTON (evolutionary stages). In the short term (around two weeks of regular local treatment), the most obvious effects demonstrate: - a clear fall prevention (antigenogenic) activity, which could have been confirmed by the realization of a trichogram practiced before and after, and during the treatment, but in the state of our means, such a technique could not be implemented artwork.

- a concomitant anti-seborrheic activity: the scalp is rid of its shiny appearance, just as the lesions of seborrheic dermatitis (dandruff condition, dry eczematiform lesions, erythematosquamous lesions) linked to sebaceous hypersecretion disappear. This effect is evidenced by a decrease in the frequency of shampoos and, importantly, does not lead to dream hypersecretion, as is often the case when the subject is forced to wash their hair at close intervals (more than 3 to 4 times per week) . In our practice, in fact, the rate of applications has remained constant and even has been reduced to just one per day without observing such a drawback.

- a stimulating activity on regrowth (anagen activity) with the appearance of downs of firm texture and well rooted in the scalp, as opposed to downs initiated during treatment with Minoxidil or Finasteride with a devitalized appearance and which do not resist not tensile. This new hair, ranging in color from white to light blonde, is preferentially born at the edge of the residual hair crown (the Hippocratic crown) and progresses centripetally. The distribution of this regrowth is not uniform, however, with a very fine down noticeable only on a curly day contrasting with longer, more pigmented and instantly visible downs. This observation illustrates well the mosaic aspect of the physiological growth of the hair in the human species.

In the medium term (around 3 months), the acquired profit persists; newly formed hair experiences regular growth, but keeps a disparity in its length and in its distribution, which at this stage obliges to resort to the hairdresser for esthetic concern. Here, it is particularly interesting, in our opinion, to point out at least two facts: - one notes the presence, during the touching of the scalp, of fine granulations of the size of a grain of sand which are, as expelled , from orifices of deserted pilosebaceous follicles;

- the appearance in scattered foci of fine punctuations of the size of a pinhead from where young hair of firm texture and more pronounced pigmentation emerge.

It is through such materialization that a regrowth begins and suggests an excellent result in the longer term. In our experience, new hair does not undergo premature involution, after being cut, it normally grows back like healthy hair.

Given the pathophysiology of alopecia, as described above, it is permissible to suggest that the lotion can have a modulating effect on the response of the pilosebaceous follicle to hormonal stress: a. an action on the transport of testosterone in particular by increasing its fixation with SHG is unlikely since the active ingredients are applied locally. The level of hormone binding to protein carrier is already determined before its reception at the follicle level. b. An especially antagonistic action at the level of the membrane receptor of testosterone before an intra-cellular passage and its transformation into DHT (DIHYDROTESTOSTERONE) by 5alpha-reductase. vs. An equally plausible action on the activity of 5alpha-reductase and directly by restoring its activity, within physiological limits (at normal level). d. Finally, a modulating action which could take place at the level of the cell nucleus, when the nuclear accepting hormone complex, penetrates there to express the hormonal message. It can be seen that the lotion applied to the face is accompanied by local beneficial effects: a. A decrease in sebaceous secretion resulting in a less shiny complexion, an attenuation of the intensity of expression lines (forehead, nasolabial folds). The whole is accompanied by a feeling of freshness in general. b. Other positive effects are also noted, testifying to a gradual systemic passage of the product: improvement in physical and intellectual performance; increased libido; reduction in intellectual fatigability thresholds; better adaptation to everyday stress. These effects were spontaneously reported by subjects experimenting with the lotion. vs. With a pure vegetable oil as an excipient, the complex can also be used as a local genital stimulant, applied to the testicles and the penis. This revitalizing side led us to create a modular complex allowing to adapt the composition, according to the site of application, to widen and to diversify its therapeutic field of application: regeneration of epidermis, stimulation of venous circulation , oral care, aphrodisiac remedy.

MODULAR VERSIONS.

1 ° Dermatological lotion for skin regeneration: SANTALINUS TM (20%) + SASSAFRAS TM (20%) + ROSMARINUS TM (5%) + CUPRESSUS SEMPERVIRENS (5%) + GINGKO BILOBAA (250 drops / 250 ml) + one excipient at 50%: a pure plant oil: ROSIER MUSCAT or CAMELIA JAPONICA or others. Use: "topical application" on the face, neck, torso or bust.

This combination allows cellular regeneration of the skin: "lifting" effect; fresher complexion; regularization of sebaceous secretions; reduction of surface wrinkles. Colateral effects are marked by analeptic and psychoanaleptic actions: improvement of organic vitality; increased libido; significant dynamism and less tiredness; better psycho-emotional comfort; improved resistance to stresses and attacks from everyday life.

2 ° Lotion stimulating the venous circulation: SANTALINUS TM (20%) + SASSAFRAS TM (20%) + ROSMARINUS T.. (5%) + GINGKO BILOBA (250 drops / 250ml) + RUSCUS ACULEATUS TM (250 drops / 250 ml) + AESCULUS HIPPOCASTANUM TM + CITRUS LIMONUM TM (250 drops / 250 ml) + a 50% excipient: a plant oil pure: Evening primrose or HEMP oil or other. Use: "topical application" on the legs.

This composition boosts blood circulation in the veins, makes the legs lighter, significantly increases muscle performance and resistance to fatigue. The side effects are marked by strong psychoanaleptic analeptic actions: improvement of the organic vitality, an increase in the libido, an important dynamism and a less fatigability, a better psychoaffective comfort, an improvement of the resistance to stresses and aggressions of life common. 3 ° Solution for oral care: SANTALINUS T.. (80%) + SASSAFRAS T.M. (5%) + ROSMARINUS T.M. (5%). + EQUISETUM HIEMALE T.M. (5%) + ABIES PECTINA T.M. (5%). Use: additive for toothpaste and drops for mouthwash solution. A few drops of this lotion on a toothpaste give the teeth a bright whiteness while regenerating the enamel which becomes smoother and cleanses the gums. Can also be used, in solution, for mouthwashes.

4 ° Aphrodisiac lotion: SANTALINUS T.M. (25%) + SASSAFRAS T.. (10%) + DAMIANA TM (10%) + GINSENG TM (5%) + GINGKO TM (5%) + CUPRESSUS TM (5%) + POPULUS NIGRA TM (5%) + AVENA SATIVA TM (5%) + KAWA - KAWA TM (5%) + an excipient: 25% pure plant oil: ONAGRE or others. Use: in topical application on the genitals. This lotion is characterized by strong effects: mild euphoric action; increased libido; better quality of erection; increased male and female desire and pleasure. No side effects have been reported or noticed.

Claims

R E V E ND I C A T I O N S

1 - Modular phyto-homeopathic complex for dermatological use comprising a plurality of tinctures, characterized in that said plurality comprises at least one mother tincture of Santalinus and one mother tincture of Sassafras officinalis, and an excipient.

2 - Complex according to claim 1, characterized in that it comprises approximately 20% of each of the two so-called mother tinctures, approximately 50% of an excipient, the rest consisting of other adjuvant dyes.

3 - Complex according to claim 1 or 2, characterized in that it comprises at least one adjuvant tincture chosen from the group comprising the following mother tinctures: Rosmarinus, Arctium Lappa, Cupressus Sempervirens, Ginkgo Biloba, Ruscus Aculeatus, Rosmarinus, Equisetum Hiemale , Damiana, Ginseng, Populus Nigra, Avena Sativa, Abies Pectina, Ka a-Ka a, and the combination thereof.

4 - Complex according to any one of the preceding claims, characterized in that the said excipient is a pure vegetable oil. 5 - Complex according to claim 4, characterized in that said oil is chosen from the group of oils obtained from Muscat rose, Camellia Japonica, Evening primrose, Hemp, or a combination thereof.

6 - Complex according to any one of the preceding claims, characterized in that it is used as a lotion.