CN1137750A - Concentrated mouthrinse for efficient delivery of antimicrobials - Google Patents
Concentrated mouthrinse for efficient delivery of antimicrobials Download PDFInfo
- Publication number
- CN1137750A CN1137750A CN 94194545 CN94194545A CN1137750A CN 1137750 A CN1137750 A CN 1137750A CN 94194545 CN94194545 CN 94194545 CN 94194545 A CN94194545 A CN 94194545A CN 1137750 A CN1137750 A CN 1137750A
- Authority
- CN
- China
- Prior art keywords
- oral cavity
- water
- composition
- antibacterial
- feature
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/347—Phenols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/41—Amines
- A61K8/416—Quaternary ammonium compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/43—Guanidines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
- A61K8/4926—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings
Abstract
Concentrated mouthrinse, methods of use and methods of manufacturing the mouthrinse for efficient delivery of cationic and water-insoluble noncationic antimicrobials wherein the composition is concentrated and substantially free of non-cationic surfactants.
Description
Technical field
The present invention relates to a kind of concentrated mouthrinse and use thereof and manufacture method, it can be efficiently to the oral cavity delivery of antimicrobials, thereby reduces oral cavity bacterium, halitosis, and then improves oral hygiene.
Background of invention
Dental plaque in the oral cavity is a kind of organic mixture that contains viable bacteria.Antibacterial in the dental plaque can secrete acid, enzyme and microbial toxin, and these materials can cause dental caries, halitosis and gingivitis and so on periodontal disease.A premium properties that has been found that compositions of the present invention is to form spissated and makes us the collutory of feeling happy.The invention provides a kind of system, utilize it can after dilution, discharge the antibacterial of relatively low concentration efficiently to the oral cavity.Except delivery of antimicrobials, find that also this system can discharge spice efficiently.Thus, when cationic surface active agent nothing but, also have good mouthfeel and breath freshening sense, also can efficiently discharge antibacterial, thereby improve oral hygiene with effective bactericidal activity.
In the reasonable time that the understanding of using collutory to reduce or eliminate oral cavity flora being had.The example of existing list of references has: February in 1991 Charbonneau on the 19th etc. United States Patent (USP) 4,994,262; May nineteen ninety Wuelknitz on the 8th etc. United States Patent (USP) 4,923,685; June in 1989 Michaels on the 13rd United States Patent (USP) 4,839,158; April in 1989 Wagner on the 25th United States Patent (USP) 4,824,661; January in 1988 Frosch on the 12nd United States Patent (USP) 4,719,100; The United States Patent (USP) 4,716,035 of December in 1987 Sampathkumar on the 29th; August in 1986 Hayashi on the 19th etc. United States Patent (USP) 4,606,911; June in 1985 Raaf on the 25th United States Patent (USP) 4,525,343; April 6 nineteen eighty-two Parran, the United States Patent (USP) 4,323,551 of Jr; January nineteen eighty-two Melsheimer on the 26th United States Patent (USP) 4,312,889; May in 1979 Pader on the 1st United States Patent (USP) 4,152,418; May in 1978 Pader on the 4th United States Patent (USP) 4,082,841; October in 1976 Benedict on the 26th United States Patent (USP) 3,988,433; May in 1976 Prussin on the 4th United States Patent (USP) 3,954,962; February in 1971 Griebstein on the 2nd etc. United States Patent (USP) 3,560,608.
The compositions that proposes in above-mentioned United States Patent (USP), other lists of references have disclosed the collutory that the oral cavity is used.For example: the belgian patent 776,425 of the Imperial Chemi-cal Industries Limited that announces on June 8th, 1972; The Canadian Patent 1081-127 that announces on July 8th, 1980; Clear and the 54008-713 of Japanese publication that announces on January 23rd, 1979; Clear and the 49007-440 of Japanese publication that announces on January 23rd, 1974; The Russian Patent 874-061 of the Krasd Perfume Works that announces on October 5th, 1981; The Russian Patent application 740-248 (with the United States Patent (USP) 3,591 of Brilliant on the 6th July in 1971,675 is similar) of the Mosc SvobodaCosmetics that announces on June 6th, 1980.
Though in collutory, used antibacterial for a long time, but still needed the acceptance that other prescription improves the performance of its opposing oral disease and improves user.
The present invention relates to be dissolved in the compositions that contains some solvent, cationic antiseptic and non-cationic type antibacterial in certain concentrated solution that makes us feeling happy.This collutory can be with water dilution to provide the safe and effective procedure that reduces oral cavity bacterium and to certain curative effect signal of user.Compare with the ready-made collutory of routine, antibacterial of the present invention and the spice release efficiency when using similar concentration is higher.
So, one of purpose of the present invention provide a kind of spissated, make us feeling happy collutory, though similar in the working concentration of antibacterial and spice and the ready-made collutory wherein, their release when release is more effective.
Another object of the present invention provides the improved collutory compositions of antiplaque effect.
A further object of the present invention provides the safe and effective procedure that is prepared collutory by concentrated solution.
Specify by following, it will be more apparent more than reaching other purpose.
Summary of the invention
The present invention relates to not carbonated, spissated, oil in water emulsion compositions, this based composition is suitable for use as collutory, wherein contains:
(a) cationic antiseptic of safe and effective amount;
(b) water-insoluble of safe and effective amount, non-cationic type antibacterial;
(c) solvent that is applicable to the oral cavity of safe and effective amount;
(d) spice of safe and effective amount; With
(e) water
The pH of compositions is about 5 to 8, and compositions does not contain anionic and nonionic surfactant substantially, and wherein said oil in water emulsion can breakdown of emulsion after diluting with certain aqueous solution that is higher than about 5%v/v.The present invention has also disclosed using method.
Unless otherwise mentioned, concentration herein and ratio all by weight, all mensuration is all carried out at 25 ℃.
Of the present invention specifying
" safe and effective amount " herein is meant to be enough to reduce oral cavity bacterium and/or to strengthen this minimizing effect but to the consumption of the no ill effect of soft or hard tissue in oral cavity.
Herein " not containing anionic surfactant substantially " is meant and is less than 0.05%, to be less than 0.01% for good, certain anionic surfactant most preferably less than 0.001%.Be meant the activity that does not weaken cationic surface active agent basically " not containing nonionic surfactant substantially " herein.Usually, it is about 0.5% that this shows that the content of the nonionic surfactant in the compositions must be lower than, and to be lower than 0.3% for good, is preferably lower than 0.2%.
Compositions of the present invention has been used a kind of cationic antiseptic, certain water-insoluble non-cationic type antibacterial, certain solvent or solvent mixture, certain spice or spice mixt and water.Concentrated mouthrinse is preferably clarifying." clarification " herein is not meant colourless, but basically less than the granule that makes it even as big as scatter visible light to be estimated.
During use, concentrated solution is mixed with the water of requirement.This mixing makes being separated at once before use.No matter how to say in theory it is believed that it is that this being separated produced the efficient release of capacity antibacterial, produce best mouthfeel and impression simultaneously.
The water yield that adds in the concentrated mouthrinse mixture must be enough to produce phase transformation as described below.This phase transformation is easy to be observed by user in dilution, and provides an operable visible signal of said composition to user.
No matter how to say in theory, it is believed that in dilution along with mixing of oil phase and water, highly water-insoluble essential oil becomes at the aqueous phase of stand-by collutory and is uniformly dispersed.With the blended water-insoluble non-cationic type antibacterial of the present invention of essential oil also be scattered in fully in the same way this mutually in.Cationic antiseptic among the present invention has the inherent character of hydrophobic and hydrophilic segment simultaneously and mainly rests on oil-water interface owing to it.Specifically, the hydrophobic part of cationic antiseptic rests in the dispersive oil phase of biphase mixture, and the charged hydrophilic segment of cationic antiseptic is enclosed in the surface (or oil-water interface) of little oil droplet, has formed countless micelle microgranules thus.Be exactly the formation of this biphase mixture, and especially cationic antiseptic is positioned at oil-in-water interface, has caused the efficient release of antibacterial among the present invention.Except the bactericidal activity of cationic antiseptic, it also plays the Magnetic force tracting effect, and the micelle component that comprises water-insoluble non-cationic type antibacterial is transmitted to the oral mucosa surface of oppositely charged.This also causes more effective release of water-insoluble non-cationic type antibacterial.So though the structure of water-insoluble non-cationic type antibacterial can not guarantee that its originally just rests on oil-water interface, it is therefore mechanism and being benefited still.
This being separated, oil phase wherein is dispersed in the aqueous phase of the collutory after the dilution, can keep a few hours.But oil phase is coalescent to become isolating one deck.So, do not dilute more than the concentrated solution of use amount immediately.
The pH of concentrate composition is about 5.0 to 8.0 among the present invention, about 6.5 to 7.0 to be good, is the best with about 6.9.Essential component and optional component in the present composition are as described below.
Essential component
Cationic antiseptic
The cationic antiseptic that is used for the present composition can be selected from quaternary ammonium compound and replace guanidine class and corresponding compounds alexidine (alexidine) thereof as chlorhexidine etc.Also can use the mixture of these cationic antiseptics among the present invention.
Those that germ-resistant quaternary ammonium compound is included, the carbochain of one or two in the substituent group on its quaternary nitrogen atoms (being generally alkyl) is about 8 to 20, usually be about 10 to 18 carbon atoms, and all the other substituent groups (being generally alkyl or benzyl) carbon number is less, 1 to 7 carbon atom, normally methyl or ethyl according to appointment.Typical quaternary amines antibacterial example has the bromination dodecyl trimethyl ammonium, TPC, domiphen bromide, chlorination N-myristyl-4-ethylpyridine, bromination dodecyl dimethyl (2-benzyloxy ethyl) ammonium, zephiran chloride dimethyl stearyl ammonium, cetylpyridinium chloride (cetylpyridinium chloride), quaternised 5-amino-1, two (2-the ethylhexyl)-5-methyl hexahydropyrimidines of 3-, benzalkonium chloride, benzethonium chloride and methylbenzethonium chloride.Other chemical compound is also just like the Bailey that quotes as proof at this United States Patent (USP) 4,206,215 described two (4-(R-amino)-1-pyridine) paraffinic on June 3rd, 1980.Preferably pyridine quaternary ammonium compound, most preferably cetylpyridinium chloride or TPC.Quaternary amines antibacterial content in the present invention is about 0.05% to 10.0%, and about 0.2% to 3.0% to be good, about 0.5% to 3.0% is better, about 0.5% to 2.0% the best.
Replace the guanidine class and also be applicable to the present invention.The preferred bis-biguanide compounds of the present invention has following general structure:
A wherein and A ' can be that (1) can optionally be contained 1 alkyl or alkoxyl to about 4 carbon atoms by one, a nitro or the phenyl that halogen atom replaces; (2) contain the alkyl of about 1 to 12 carbon atom; Or (3) contain the alcyl of about 4 to 12 carbon atoms; X wherein and X ' represent an alkylidene that contains about 1 to 3 carbon atom separately; Z wherein and Z ' can be respectively 0 or 1; R wherein and R ' respectively represent hydrogen atom, contain the alkyl of about 1 to 12 carbon atom, or contain the aralkyl of about 7 to 12 carbon atoms; N wherein is the integer of 2 to 12 (comprising end value); Polymethylene chain (CH wherein
2)
nCan optionally be interrupted by oxygen atom, sulphur atom or aromatic proton.Especially preferably use the water soluble salt of above-claimed cpd at this.Suitable water soluble salt has chloride, fluoride, especially acetate.Preferred replacement guanidine is chlorhexidine-(1,6 couple of (N
5-rubigan-N-biguanide base) hexane).The consumption that replaces guanidine among the present invention is about 0.05% to 3.0%, about 0.5% to 3.0% to be good, is the best with about 0.5% to 2.0%.
Water-insoluble non-cationic type antibacterial
Second must component be water-insoluble non-cationic type antibacterial.It below is the example that is used for water-insoluble non-cationic type antibacterial of the present invention.
Halogenated diphenyl ethers 2 ', 4,4 '-three chloro-2-dihydroxy diphenyl ethers (triclosan) 2,2 '-dihydroxy-5,5 '-dibromodiphenyl ether
Phenolic compound (comprising phenol and homologue thereof, monoalkyl, many alkyl and aromatic halophenol, resorcinol and derivant thereof, bisphenol compound and halogenation salicylamide)
Phenol and homologue phenol 5-methyl-2-(1-Methylethyl) phenol (thymol) 2-methylphenol 3-methylphenol 4-methylphenol 4-ethyl-phenol 2 thereof, 4-xylenol 2,5-xylenol 3,4-xylenol 2,6-xylenol 4-n-pro-pyl phenol 4-normal-butyl phenol 4-n-pentyl phenol 4-tert-amyl phenol 4-n-hexyl phenol 4-n-heptyl phenol
Monoalkyl, the adjacent benzyl of methyl parachlorophenol between the adjacent benzyl of the adjacent benzyl parachlorophenol of many alkyl and aromatic series halophenol parachlorophenol methyl parachlorophenol ethyl parachlorophenol n-pro-pyl parachlorophenol normal-butyl parachlorophenol n-pentyl parachlorophenol sec-amyl parachlorophenol n-hexyl parachlorophenol cyclohexyl parachlorophenol n-heptyl parachlorophenol n-octyl parachlorophenol o-chlorphenol methyl o-chlorphenol ethyl o-chlorphenol n-pro-pyl o-chlorphenol normal-butyl o-chlorphenol n-pentyl o-chlorphenol tertiary pentyl o-chlorphenol n-hexyl o-chlorphenol n-heptyl o-chlorphenol-, between-the adjacent phenethyl of the adjacent phenethyl parachlorophenol of dimethyl parachlorophenol between methyl parachlorophenol 3-methyl parachlorophenol 3,5-dimethyl parachlorophenol 6-ethyl-3-methyl-parachlorophenol 6-n-pro-pyl-3-methyl-parachlorophenol 6-isopropyl-3-methyl-parachlorophenol 2-ethyl-3,5-dimethyl-parachlorophenol 6-sec-butyl-3-methyl-parachlorophenol 2-isopropyl-3,5-dimethyl-parachlorophenol 6-diethylmethyl-3-methyl-parachlorophenol 6-isopropyl-2-ethyl-3-methyl-parachlorophenol 2-sec-amyl-3,5-dimethyl-parachlorophenol 2-diethylmethyl-3, the adjacent bromophenol n-pro-pyl of the adjacent bromophenol n-hexyl of the adjacent bromophenol tertiary pentyl of 5-dimethyl-parachlorophenol 6-secondary octyl-3-methyl-parachlorophenol p bromophenol methyl p bromophenol ethyl p bromophenol n-pro-pyl p bromophenol normal-butyl p bromophenol n-pentyl p bromophenol sec-amyl p bromophenol n-hexyl p bromophenol cyclohexyl p bromophenol-, between-dimethyl-adjacent bromophenol 2-phenylphenol 4-chloro-2-methylphenol 4-chloro-3-methylphenol 4-chloro-3,5-xylenol 2,4-two chloro-3,5-xylenol 3,4,5,6-tetrabromobisphenol-methylphenol 5-methyl-2-amyl phenol 4-isopropyl-3-methylphenol 5-chloro-2-hydroxy diphenyl methane
Resorcinol and derivant resorcinol methylresorcinol ethyl resorcinol n-pro-pyl resorcinol n-butyl resorcinol n-pentyl resorcinol n-hexyl resorcinol (n=4 thereof, hexylresorcinol) n-heptyl resorcinol n-octyl resorcinol n-nonyl resorcinol phenyl resorcinol benzyl resorcinol phenethyl resorcinol arylate base resorcinol p-chlorobenzyl resorcinol 5-chloro-2,4-dihydroxy diphenyl methane 4 '-chloro-2,4-dihydroxy diphenyl methane 5-bromo-2,4-dihydroxy diphenyl methane 4 '-bromo-2,4-dihydroxy diphenyl methane
Bisphenol compound 2,2 '-di-2-ethylhexylphosphine oxide (4-chlorophenol) 2,2 '-di-2-ethylhexylphosphine oxide (3,4, the 6-trichlorophenol, 2,4,6,-T) 2, two (2-hydroxyl-5-benzyl chloride base) thioethers of 2 '-di-2-ethylhexylphosphine oxide (4-chloro-6-bromophenol) two (2-hydroxyl-3,5-Dichlorobenzene base) thioether
Halogenation salicylamide 4 ', 5-two bromo-salicylamides 3,4 ', 5-three chloro-salicylamides 3,4 ', 5-three bromo-salicylamides 2,3,3 ', 5-tetrachloro-salicylamide 3,3 ', 5-three chloro-salicylamides 3, the 5-two bromo-3 '-trifluoromethyl-positive decoyl-3 ' of salicylamide 5--trifluoromethyl-salicylamide 3,5-two bromo-4 '-trifluoromethyl-salicylamide 3,5-two bromo-3 '-trifluoromethyl-salicylamide (fluorosalan)
Benzoate P-hydroxybenzoic acid methyl parahydroxybenzoate ethylparaben propyl p-hydroxybenzoate butyl p-hydroxybenzoate
Halogenation carbanilide 3,4,4 '-three chloro-carbanilide 3-trifluoromethyls-4,4 '-two chloro-carbanilides 3,3 ', 4-three chloro-carbanilides
No matter how theory is said, it is believed that distinctive cationic and combination water-insoluble non-cationic type antibacterial that is dispersed in the oil-in-water emulsion of the present invention has improved the effect of antiplaque.Especially, water-insoluble non-cationic type antibacterial it is believed that and can arrive the not readily accessible bacterium colony that is positioned at dental plaque of cationic antiseptic.So no matter the aggregation degree of existing dental plaque is how, the new combination results of this two classes antibacterial a kind ofly provide effective antiplaque active potent antiplaque compositions.
Containing the water-insoluble non-cationic antimicrobial agent of effective antiplaque amount in the composition for oral cavity by the preparation of the application's method, be generally about 0.01-5% (weight), is good with about 0.03-1%.Water insoluble substantially its dissolubility in 25 ℃ water that means of antibacterial is less than 1% (weight), even may be less than 0.1%.If ionogenic group is arranged, the mensuration of dissolubility should be carried out under the ionized pH of a unlikely generation.
Solvent or solvent system
The another kind of the present composition must composition be certain solvent or solvent system, as the United States Patent (USP) 5,141,961 in Coapman on August 25th, 1992 of quoting as proof at this described those.Account for the carrier that most this (a bit) solvent of the present composition plays a part Oleum sesami.This solvent or solvent system make essential oil be dissolved in the concentrated solution and help oil-soluble components all in the concentrate formulation to disperse behind thin up, form a homodisperse mixture thus.Most preferably being used for solvent of the present invention is: Polyethylene Glycol, propylene glycol, butanediol and hexanediol or their mixture.Propylene glycol most preferably.
Propylene glycol is that this specialty is known, and many suppliers are arranged.Polypropylene glycol can be arbitrarily than dissolving each other with water, and the spice among solubilized the present invention.Be applicable to that propylene glycol of the present invention can derive from the arbitrary family among many suppliers, as Dow Chemical.Polyethylene Glycol also is that this specialty is known, and the product of lower molecular weight has and the propylene glycol similar characteristic.The mean molecule quantity that is applicable to Polyethylene Glycol of the present invention is less than or equal to 600, as the PEG 300 " Carbowax " that is provided by Union Carbide.
Solvent accounts for the about 30% to 90% of collutory conc forms, about 35% to 80% to be good, is the best with about 45% to 80%.
Contain water in the concentrate composition of the present invention.Water accounts for the about 10% to 40% of composition for oral cavity described herein, refers to that with about 10% 30% is good, is the best with about 10% to 25%.The water of these quantity comprises that the free water of adding adds the water of bringing into other material such as sorbitol.Be used for preferably deionized-distilled water of water of the present invention, do not contain organic impurity and antibacterial, and metal ion not substantially.
Spice
Another kind of the present invention must component be the mixture of spice or compatible spice.This class spice is that this specialty is known.Suitable spice has: Fructus Foeniculi, Cortex Cinnamomi, clove tree, dihydroanethole, estragole, alcohol, Herba Menthae, oxanone, phenylethanol, Betula lenta, thymol, acetaminol, cineole, wintergreen oil, Mentha viridis L, cinnamic aldehyde, ketone, α-ionone, ethyl vanillin, limonene, isoamyl acetate, benzaldehyde, ethyl n-butyrate. is many with other.Perfumes comprise is about 0.2% to 9.0% in compositions as herein described, about 0.6% to 4.0% to be good, is the best with 2.0% to 4.0%.
Optional component
Being used for of the present invention one optional component is the mixture of wetting agent or compatible wetting agent.Wetting agent is that this specialty is known.Wetting agent suitable among the present invention has xylitol, the mixture of polyhydric alcohol such as glycerol and sorbitol and these wetting agents.Though can use single wetting agent, be good to use the mixing wetting agent.Wetting agent accounts for approximately 0% to 55% in the present invention, preferably accounts for 15% to 30%.The preferred wetting agent that mixes was had an appointment preferably about 3: 1 to 1: 2 glycerol and sorbitol 10: 1 to 1: 4.
Other optional component includes but not limited to: the color element; Sweeting agent has glucide, glucose, fructose, and cyclamate and aspartame and other are many; Buffer agent is as benzoic acid and sodium benzoate, citric acid and sodium citrate and the compatible buffer of other component any and required in this invention.Another optional component of the present invention is an ethanol.Ethanol has multinomial function when being blended in the compositions of the present invention.Comprising but be not limited to as additional antibacterial or astringent.Alcoholic acid content can be less than approximately 40% among the present invention, to be less than about 10% for good, is the best to be less than 2% in concentrated solution.
Other optional component of the present invention also has freshener, United States Patent (USP) 4 as Wat-son on the 23rd etc. January in 1979,136,163,1980 on October 28, Rowsell etc. United States Patent (USP) 4,230,668 and the United States Patent (USP) 4 of Rowsell etc., described in 023,661 those, above document all is hereby incorporated by reference.Most preferred a kind of freshener be the N-ethyl to alkane 3-Methanamide (WS-3 that Sterling Organics provides), by the United States Patent (USP) 4,136 of reference, 163 is described as above.
Preparation method
Desire effectively the present invention as the sterilization collutory, user must face with preceding by adding aqueous solution (preferably water) in spissated oil-in-water emulsion, or oil-in-water emulsion added in the entry is prepared.After the dilution, the oil-in-water emulsion breakdown of emulsion discharges the muddiness (or opaque materials) that is formed by diluted compositions.This usually occurs in Emulsion and to add greater than 5%v/v, about 10% being good, when being the aqueous solution of the best with about 20%.So after the dilution, the compositions of formation is not fully transparent.But this transformation visual observations, or utilize a spectrophotometer to record easily.Any significant difference of the concentrated solution absorbance after undiluted concentrated solution and the dilution shows the interaction and the diffusion of the light of the present invention's needs, and it has constituted the scope of " turbidity ".Do not need other stirrings and blended energy to realize disperseing fast to form antibacterial among the present invention, the homodisperse mixed stocker of essential oil and other component.The dilution of concentrated mouthrinse requires the mixing ratio of concentrated solution and water to be about 1: 1 to 1: 100, with about 1: 20 to 1: 50 be good, about 1: 5 to 1: 50 is better, about 1: 20 to 1: 50 the best.
The use of compositions
The present invention relates to gargling with the collutory of safe and effective amount with regard to its method aspect and washes the oral cavity, and collutory is made by diluting concentrated solution as herein described with an amount of water by user.Usually, by above-mentioned dilution, at least about the antibacterial that contains 0.01g, the flora that exists in the oral cavity can be eliminated or reduce to these antibacterial effectively in the collutory.
Manufacture method
The manufacture method of disclosed compositions is very common in the oral cavity with product scope.
Following examples have further described and have illustrated the preferred embodiment in the scope of the invention.These embodiment only provide for the purpose of description, and should not be considered to be limited field of the present invention, because many changes that do not deviate from aim of the present invention and scope can be arranged.
Example I
The following composition of following mixing prepares concentrated mouthrinse of the present invention.Provide the dilution gfactor of this concentrated solution of dilution simultaneously.
Thinner ratio (concentrated solution: water)=1: 39
Cetylpyridinium chloride 2.000%
Triclosan 3.0000%
Propylene glycol 77.0000%
Water 11.0000%
Spice 3.0000%
WS-3* 1.0000％
Saccharin sodium 3.0000%*N-ethyl-to alkane-3-Methanamide, by Wilkinson-Sword, Inc. provides
In rustless steel that contains a certain amount of solvent or glass blending tank, add in turn and the following composition of stirring and dissolving: spice, freshener, benzoic acid, antibacterial, wetting agent, pure water, sodium benzoate, sweeting agent and pigment.
User needs to add 39 parts of water in above-mentioned concentrated solution.
It is muddy that compositions after the dilution will become, and this collutory of prompting user can use.Then, the compositions of user after with the dilution of about 20ml spues after gargling and washing the oral cavity again.So can reduce or eliminate the antibacterial in the oral cavity, prevention of gingivitis and other oral disease.Can obtain substantially the same effect with the antibacterial of enumerating more than all or part of replacement of following antibacterial: the bromination dodecyl trimethyl ammonium, TPC, domiphen bromide, chlorination N-myristyl-4-ethylpyridine, bromination dodecyl dimethyl (2-phenoxy group ethyl) ammonium, zephiran chloride dimethyl stearyl ammonium, cetylpyridinium chloride (cetylpyridinium chloride), quaternised 5-amino-1, two (2-the ethylhexyl)-5-methyl hexahydropyrimidines of 3-, benzalkonium chloride, benzethonium chloride and methylbenzethonium chloride or other any one at the antibacterial of this explanation.
Example II
Thinner ratio (concentrated solution: water)=1: 39
Cetylpyridinium chloride 2.000%
Thymol 2.0000%
Propylene glycol 75.0000%
Water 14.5000%
Spice 3.0000%
WS-3 0.5000％
Saccharin sodium 3.0000%
EXAMPLE III
Thinner ratio (concentrated solution: water)=1: 9
Cetylpyridinium chloride 0.5000%
Thymol 0.5000%
Propylene glycol 70.0000%
Water 27.3000%
Spice 1.0000%
Saccharin sodium 0.7000%
The manufacture method of compositions and example I are basic identical among example II and the III.
Claims (10)
1. the not carbonated concentrated composition for oral cavity of an oil-in-water emulsion form is characterized in that it contains:
(a) certain cationic antiseptic of 0.05% to 10.0%;
(b) certain water-insoluble non-cationic type antibacterial of 0.05% to 10.0%;
(c) 30% to 90% the mouth solvent of safety;
(d) 0.2% to 9.0% spice; And
(e) pH of 10% to 40% water composition is 5 to 8, and compositions is substantially free of anionic and nonionic surfactant, and when certain aqueous solution dilution of using greater than 5%v/v, described oil-in-water emulsion is breakdown of emulsion immediately.
2. composition for oral cavity according to claim 1, its feature are that also antibacterial wherein is selected from quaternary amines antibacterial such as cetylpyridinium chloride (cetylpyridinium chloride), TPC and composition thereof.
3. according to the described composition for oral cavity of arbitrary aforementioned claim, its feature is that also quaternary amines antibacterial content wherein is 0.5% to 3.0%.
4. according to the described composition for oral cavity of arbitrary aforementioned claim, its feature is that also water-insoluble non-cationic type antibacterial wherein is selected from thymol, phenol, hexylresorcinol, triclosan and composition thereof.
5. according to the described composition for oral cavity of arbitrary aforementioned claim, its feature is that also water-insoluble non-cationic type antibacterial wherein is a triclosan.
6. according to the described composition for oral cavity of arbitrary aforementioned claim, its feature is that also solvent wherein is 40% to 80%.
7. according to the described composition for oral cavity of arbitrary aforementioned claim, its feature is that also solvent wherein is selected from propylene glycol, Polyethylene Glycol, butanediol, hexanediol and composition thereof.
8. according to the described composition for oral cavity of arbitrary aforementioned claim, its feature is that also wherein flavour content is 0.6% to 4.0%.
9. according to the described composition for oral cavity of arbitrary aforementioned claim, its feature also is, wherein also contains 5.0% to 55.0% wetting agent that is selected from glycerol, sorbitol and composition thereof.
10. according to the described composition for oral cavity of arbitrary aforementioned claim, its feature also is, wherein also contains 0% to 20% ethanol.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17157693A | 1993-12-22 | 1993-12-22 | |
| US08/171,576 | 1993-12-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1137750A true CN1137750A (en) | 1996-12-11 |
Family
ID=22624283
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 94194545 Pending CN1137750A (en) | 1993-12-22 | 1994-12-21 | Concentrated mouthrinse for efficient delivery of antimicrobials |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP0735856A1 (en) |
| JP (1) | JPH09510186A (en) |
| CN (1) | CN1137750A (en) |
| PE (1) | PE44595A1 (en) |
| WO (1) | WO1995017159A1 (en) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1297252C (en) * | 2000-01-31 | 2007-01-31 | 阿肯色州大学 | Concentrated solution of non-foaming ammonium compounds and method of use |
| CN103025266A (en) * | 2010-07-30 | 2013-04-03 | 高露洁-棕榄公司 | Mouthwash formulations for use with toothbrush delivery device |
| CN103190962A (en) * | 2012-01-04 | 2013-07-10 | 江苏雪豹日化有限公司 | Manufacturing method of oral sponge cleaning stick |
| CN103906500A (en) * | 2011-11-09 | 2014-07-02 | 高露洁-棕榄公司 | Alcohol-free mouthwash |
| CN104411290A (en) * | 2012-06-21 | 2015-03-11 | 宝洁公司 | Mouth rinse emulsions |
| CN104853734A (en) * | 2012-12-20 | 2015-08-19 | 高露洁-棕榄公司 | Oral care composition containing ionic liquids |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6440395B1 (en) | 1992-06-22 | 2002-08-27 | Barry M. Libin | Antiplaque mouth rinse |
| US5961970A (en) * | 1993-10-29 | 1999-10-05 | Pharmos Corporation | Submicron emulsions as vaccine adjuvants |
| DE69516406T2 (en) * | 1994-06-10 | 2001-01-18 | Procter & Gamble | ORAL DETERGENT |
| EP0764014A1 (en) * | 1994-06-10 | 1997-03-26 | The Procter & Gamble Company | Mouthrinse compositions |
| US5891422A (en) * | 1996-10-10 | 1999-04-06 | Warner-Lambert Company | Antimicrobial composition containing a C3 -C6 alcohol |
| US6436369B2 (en) * | 1998-12-17 | 2002-08-20 | Wm. Wrigley Jr. Company | Anti-plaque emulsions and products containing same |
| US8283135B2 (en) * | 2000-06-30 | 2012-10-09 | The Procter & Gamble Company | Oral care compositions containing combinations of anti-bacterial and host-response modulating agents |
| US9241885B2 (en) * | 2004-01-29 | 2016-01-26 | The Procter & Gamble Company | Oral care compositions comprising increased bioavailable levels of quaternary ammonium antimicrobials |
| US8517728B2 (en) | 2007-01-24 | 2013-08-27 | Colgate-Palmolive Company | Oral care implement having fluid delivery system |
| TWI392514B (en) | 2010-01-29 | 2013-04-11 | Colgate Palmolive Co | Fluoride free and anionic surfactant free dentifrice having a high micro efficacy |
| JP5804307B2 (en) * | 2010-03-03 | 2015-11-04 | サンスター株式会社 | Oral composition |
| MX341247B (en) | 2011-03-09 | 2016-08-12 | Colgate Palmolive Co | Interdental cleaning device. |
| EP2911554B1 (en) | 2012-10-26 | 2017-04-26 | Colgate-Palmolive Company | Oral care implement |
| WO2019174277A1 (en) * | 2018-03-13 | 2019-09-19 | The Hong Kong Polytechnic University | Phosphoethanolamine transferase inhibitors |
| CA3181110A1 (en) | 2020-06-15 | 2021-12-23 | Anindya Dasgupta | An antimicrobial composition for tackling malodour |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1365030A (en) * | 1972-11-30 | 1974-08-29 | Merck & Co Inc | Oral compositions |
| US4205061A (en) * | 1978-07-14 | 1980-05-27 | Johnson & Johnson | Oral antimicrobial compositions |
| DE3345781A1 (en) * | 1983-12-17 | 1985-06-27 | Henkel KGaA, 4000 Düsseldorf | ORAL AND DENTAL PRODUCTS |
| ZA872857B (en) * | 1986-05-02 | 1987-11-25 | Warner Lambert Co | Composition and method to inhibit the growth of organisms by the use of bis-biguanido hexanes and essential oil mixture combinations |
| US4666517A (en) * | 1986-06-04 | 1987-05-19 | Colgate-Palmolive Co. | Antiplaque oral composition |
| US4992276A (en) * | 1988-12-14 | 1991-02-12 | Warner-Lambert Company | Antiseptic compositions containing hexahydro-5-pyrimidinamine compounds and thymol and methods for preparing same |
| US5236699A (en) * | 1992-06-22 | 1993-08-17 | Libin Barry M | Antiplaque mouth rinse |
| US5405604A (en) * | 1992-10-16 | 1995-04-11 | The Procter & Gamble Company | Concentrated mouthrinse for efficient delivery of antimicrobials |
-
1994
- 1994-12-21 WO PCT/US1994/014757 patent/WO1995017159A1/en not_active Application Discontinuation
- 1994-12-21 PE PE25760194A patent/PE44595A1/en not_active Application Discontinuation
- 1994-12-21 JP JP7517586A patent/JPH09510186A/en active Pending
- 1994-12-21 CN CN 94194545 patent/CN1137750A/en active Pending
- 1994-12-21 EP EP95906064A patent/EP0735856A1/en not_active Ceased
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1297252C (en) * | 2000-01-31 | 2007-01-31 | 阿肯色州大学 | Concentrated solution of non-foaming ammonium compounds and method of use |
| CN103025266A (en) * | 2010-07-30 | 2013-04-03 | 高露洁-棕榄公司 | Mouthwash formulations for use with toothbrush delivery device |
| CN103025266B (en) * | 2010-07-30 | 2015-08-19 | 高露洁-棕榄公司 | The mouthwash formulations used together with toothbrush delivery apparatus |
| CN103906500A (en) * | 2011-11-09 | 2014-07-02 | 高露洁-棕榄公司 | Alcohol-free mouthwash |
| CN103906500B (en) * | 2011-11-09 | 2017-08-08 | 高露洁-棕榄公司 | Alcohol-free mouthwash |
| CN103190962A (en) * | 2012-01-04 | 2013-07-10 | 江苏雪豹日化有限公司 | Manufacturing method of oral sponge cleaning stick |
| CN104411290A (en) * | 2012-06-21 | 2015-03-11 | 宝洁公司 | Mouth rinse emulsions |
| CN104853734A (en) * | 2012-12-20 | 2015-08-19 | 高露洁-棕榄公司 | Oral care composition containing ionic liquids |
Also Published As
| Publication number | Publication date |
|---|---|
| WO1995017159A1 (en) | 1995-06-29 |
| JPH09510186A (en) | 1997-10-14 |
| PE44595A1 (en) | 1996-01-10 |
| EP0735856A1 (en) | 1996-10-09 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1137750A (en) | Concentrated mouthrinse for efficient delivery of antimicrobials | |
| CA2146635C (en) | Concentrated mouthrinse for efficient delivery of antimicrobials | |
| EP1171084B1 (en) | Zinc containing dentifrice compositions | |
| KR101763953B1 (en) | Composition for oral cavity | |
| CN101346125A (en) | Taste making of essential oils using a hydrocolloid | |
| FR2729050A1 (en) | Synergistic compsn. with microbicidal properties | |
| EP2961372B1 (en) | Oral care compositions | |
| JP5105059B2 (en) | Dentifrice composition | |
| KR102183186B1 (en) | Cosmetic Composition Comprising High Concentration of Vitamin C | |
| JP2005179266A (en) | Dentifrice composition | |
| JP6138538B2 (en) | Transparent liquid composition for oral cavity | |
| JPH082773B2 (en) | Rose composition | |
| US20040259958A1 (en) | Non-halogenated phenoxy and/or benzyloxy substituted phenols, antimicrobial compositions containing the same, and methods of using the same | |
| EP2531262B1 (en) | Oral care composition comprising a precursor of chlorine dioxide and lipophilic excipients | |
| CN1630506A (en) | Compositions for cleansing skin and treating acne | |
| EP2961373B1 (en) | Oral care compositions | |
| JP7236623B2 (en) | oral composition | |
| JP2009292744A (en) | Liquid composition for oral cavity | |
| JP2003342142A (en) | Composition for oral cavity | |
| JP6728300B2 (en) | Oral composition | |
| JP2017125072A (en) | Transparent liquid composition for oral cavity | |
| JP2024025295A (en) | Oral composition | |
| JP2011184412A (en) | Emulsified composition, and skin care preparation for external use containing the same | |
| JPH1179961A (en) | Composition for oral cavity | |
| DE102016203146A1 (en) | Antibacterial oral care gels |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C01 | Deemed withdrawal of patent application (patent law 1993) | ||
| WD01 | Invention patent application deemed withdrawn after publication |