MXPA96000547A - Depilatory compositions that comprise sulfohidr members - Google Patents

Abstract

The present invention involves topical depilatory compositions, at a pH of 7, comprising sulfohydride compounds. The present invention also relates to methods for removing fur from mammalian skin, comprising the topical application of a composition, at a pH of 7, comprising a sulfohydryl compound or a cosmetically and / or pharmaceutically acceptable salt of the same.

Description

DEPILATORY COMPOSITIONS COMPRISING SULFORPHYDRYL COMPOUNDS FIELD OF THE INVENTION The present invention relates to the field of hair removal from mammalian skin. Specifically, the present invention relates to methods for hair removal of human skin.

BACKGROUND OF THE INVENTION The removal of hair from the human body has received considerable attention, for both medical and cosmetic reasons. There are several methods to remove unwanted hair. Conventional methods focus on mechanical removal and chemical depilation, whereby unwanted hair is removed once it has appeared on the surface of the skin. Other methods involve the prevention, suppression or retardation of hair growth, through an alteration in the speed and character of hair growth. Mechanical methods used for hair removal include hair removal by tongs, peeling, electrolysis, razor and X-ray techniques. Hair removal and peeling are of limited utility because their use is confined to a localized area. The techniques of electrolysis and X-rays are painful and require the use of expensive equipment, while shaving induces irritation of the skin. Depilatory chemical compositions are effective in removing unwanted hair from large areas on the skin. These compositions typically break the disulfide bonds in the hair keratin, thereby causing the hair fiber to disintegrate. However, most depilatory chemical compositions are strongly alkaline, causing dermal irritation, particularly on the sensitive skin of the face. At present, compositions generally called "waxes" are also used for hair removal. These are applied to the skin in a molten state. When it cools and hardens, the wax traps the contacting hair. The wax is removed from the skin, pulling the hair trapped by its roots. Even though waxing is longer than other chemical methods, it is unfavorable because it tends to cause irritation, inflammation or possible burns. Of the methods used to alter the speed and character of hair growth, most involve the application of anti-androgens to control the dermatological conditions associated with androgen-dependent diseases, such as female hirsutism. However, these methods have undesirable side effects such as systematic ani-androgen effects, teratogenecity and pituitary dysfunctions, and are consequently of limited use. For the above reasons, there is a need to develop a method that is effective, easy to administer, non-irritating, long-lasting, and that can remove unwanted hair and / or regulate unwanted hair growth without allowing rapid return. of growth. It is an object of the present invention to provide topical compositions for removing unwanted hair from the skin of the mammal. It is also an object of the present invention to provide such compositions that are benevolent and less irritating to the skin than the existing compositions. It is also an object of the present invention to provide methods for removing hair from the skin of the mammal.

SUMMARY OF THE INVENTION The present invention involves topical compositions for removing unwanted hair, especially hair, and / or regulating hair growth in a mammal susceptible to or suffering from hirsutism or unwanted hair, comprising as an active agent a compound of sufohydryl in a pharmaceutically and / or cosmetically acceptable carrier such that the composition has a pH of 7 or less. The present invention further involves methods for removing hair and / or regulating hair growth in a susceptible mammal suffering from hirsutism or unwanted hair, which comprises applying topically to the skin of the mammal a composition that can be allowed to remain, comprising a sulfohydride compound in a pharmaceutically and / or cosmetically acceptable carrier, such that the composition has a pH of 7 or less.

DETAILED DESCRIPTION OF THE INVENTION As used herein, the term "sulfohydryl compound" means a compound having a -SH group selected from the group consisting of thioglycolic acid, cysteine, homocysteine, glutathione, thioglycerol, thiomalic acid, 2-mercaptopropionic acid, 3-mercaptopropionic acid, thiodiglycol, 2-mercaptoethanol, dithiothreitol, thioxanthane, thiosalicylic acid, thiolactic acid, thiopropionic acid, thiodiglycolic acid, N-acetyl-L-cysteine, lipoic acid, and cosmetically and / or pharmaceutically acceptable salts of any of the above compounds Mixtures of sulfohydride compounds are suitable for use herein Preferred sulfohydryl compounds include thioglycolic acid, cysteine, glutathione, N-acetyl-L-cysteine, lipoic acid, thiosalicylic acid, and thiolactic acid and cosmetic salts and / or pharmaceutically acceptable thereof.

More preferred sulfohydride compounds include thioglycolic acid, cysteine, glutathione and N-acetyl-L-cysteine, and cosmetically and / or pharmaceutically acceptable salts thereof. The most preferred sulfohydride compound is N-acetyl-L-cysteine and cosmetically and / or pharmaceutically acceptable salts thereof. As used herein, the term "cosmetically and / or pharmaceutically acceptable salts" of the sulfohydride compounds include, but are not limited to, alkali metal salts, ie, sodium, lithium, rubidium and potassium salts; salts of alkaline earth metals, that is, magnesium, calcium and strontium salts; non-toxic heavy metal salts, that is, aluminum salts or zinc salts; silicon salts; ammonium salts; trialkylammonium salts, that is, trimethylammonium and triethylammonium; and tretralkylammonium salts. Cosmetically and / or pharmaceutically acceptable salts of the preferred sulfohydryl compounds include salts of Na +, K +, Ca ++, Mg ++, Al2 (OH) 5+, NH4 +, (HOCH2CH2) 3NH +, (CH-jCl,) jNH *, (CHjCH ^ N *, C12H25 (CHJJJ * and C12H25 (C5H4N) 3N * - The most preferred salts of the sulfohydryl compounds include Na +, K *, NH4 + salts and (HOCHjCH ^ jNH *.) Salts of the most preferred sulfohydryl compounds include salts of Na + and NH4 *. Suitable salts of the sulfohydride compound are described, for example, in US Patent No. 5,269,500, issued to Hillebrand on the 22nd. March 1994, incorporated herein by reference.

It has been unexpectedly found that compositions containing sulfohydride compounds at an acidic or neutral pH, exhibit the ability to remove unwanted hair on the skin of mammals without the undesirable side effects, such as skin irritation and odor, commonly associated with known depilatory formulations. While not limited to any particular mode of action, it is believed that sulfohydride compounds remove unwanted hair by breaking the disulphide bonds present in hair keratin. Without attempting to be bound or limited by theory, the compositions of this invention can also regulate hair growth. As used herein, the term "hair" means a short, fine hair, less than 1 cm in length, that contains little or no pigmentation. The compositions herein depilate hairs because the disulfide bonds present in such hair are susceptible to cleavage by sulfohydrolysis. As used herein, the term "terminal hair" means a medullated, pigmented, thick hair that is greater than a hair. The terminal hairs are typically seen on the scalp, eyebrows and eyelashes, and include secondary sexual hair seen in the pubic region, abdomen, face and armpits.

The compositions of the invention soften the terminal hair. As used herein, the term "that may be allowed to remain" means a composition that is topically applied without being removed by washing after a given duration of time. As used herein, the term "topical application" means placing directly on or spreading on the skin of a mammal. As used here, the term "safe and effective amount" means an amount of compound or composition sufficient to significantly induce a positive modification in the condition to be treated, but sufficiently minor to avoid serious side effects (at a reasonable benefit / risk ratio) , within the scope of safe medical judgment. As may be applicable for certain uses of the present compositions, the safe and effective amount of the compound or composition will vary with the particular condition being treated, the age and physical condition of the patient being treated, the severity of the condition, the duration of the treatment, the nature of the concurrent therapy, the specific compound or composition employed, the particular cosmetic and / or pharmaceutically acceptable vehicle used, and similar factors within the knowledge and experience of a general practitioner. As used herein, the term "cosmetically and / or pharmaceutically acceptable" means that the salts, drugs, medicaments, inert ingredients or other materials that the phrase describes, are suitable for use in contact with the tissues of humans and lower animals, without undue toxicity, incompatibility, instability, irritation, allergic responses, and the like, commensurate with a reasonable benefit / risk ratio. As used herein, the term "hair growth regulation" means decreasing the hair growth rate and / or inducing the formation of fewer strands of hair, and / or decreasing the diameter of the hair filament, and / or shortening the hair filament and / or preventing, retarding, suppressing or repressing the hair growth process. The compositions of this invention preferably comprise from about 0.005% to about 25%, more preferably from about 0.1% to about 15%, even more preferably from about 0.5% to about 10%, still more preferably from about 1% to about 7% , but more preferably from about 2% to about 5%, most preferably about 2% of the sulfohydryl compound.

THE VEHICLE The compositions of the present invention comprise a solid, semi-solid or liquid cosmetically acceptable and / or pharmaceutically acceptable vehicle, which enables the sulfohydryl active agent to be delivered to the desired target at an appropriate concentration. The vehicle may itself be inert or may possess physiological or pharmaceutical benefits of its property. The active agent is topically applied to the skin of a subject in need of treatment. Topical application is preferably ensured with compositions in the form of lotions, solutions, ointments, serums, sprays, tonics, creams, tabs, cream rinses, bars, gels, mouses, pastes and the like. The topical compositions of the present invention can be formulated as liquid, for example, as a lotion, mouse or cream. Such liquid compositions can be formulated for use in combination with an applicator such as a roller ball applicator, a pad applicator, or a spray device such as an aerosol can containing propellant, or a container adapted with a pump to dispense the product. liquid, or a cloth impregnated with liquid, like a tissue towel. Alternatively, the compositions of the invention can be solid or semi-solid, for example, sticks, serums, creams or gels. Such solid or semi-solid compositions may be formulated for use in combination with an appropriate applicator or simply in a tube, jar or other convenient container. The selection of a vehicle for this purpose presents a broad spectrum of possibilities that depends on the form of the required product of the composition. The appropriate vehicles can be classified as described below. The term "topical vehicle" refers to substances that can act as diluents, dispersants, or solvents for the sulfohydride active agent which, therefore, guarantees that it can be applied to and evenly distributed over the selected target at an appropriate concentration. Topical carriers useful in compositions of the present invention may include water as a carrier, and one or more cosmetically and / or pharmaceutically acceptable carriers other than water. The topical vehicle is preferably one that can help and / or improve the penetration of the active sulfohydride agent into the skin to reach the immediate environment of the hair follicle. Useful carriers in topical compositions according to the present invention may include penetration enhancers, such as liposomes, latex networks, microspheres, cyclodextrans and various forms of microencapsulation of the active agent. A preferred amount of penetration enhancing agent is from about 1% to about 5% of the composition. Generally, the carrier is in any aqueous or organic nature, or an aqueous emulsion, and is capable of having the active sulfohydride agent dispersed or dissolved therein. The vehicle may include cosmetically and / or pharmaceutically acceptable emollients, skin penetration enhancers, coloring agents, fragrances, emulsifiers, thickening agents, and / or solvents. The topical compositions of the present invention can be formulated as a composition comprising an emollient. Such compositions typically comprise from about 1% to about 50%, preferably from about 5% to about 20%, of a cosmetically and / or pharmaceutically acceptable emollient; and a safe and effective amount of the sulfohydride active agent. As used herein, the term "emollients" refers to materials used for the prevention or aid of dryness, as well as for the protection of the skin. A wide variety of suitable emollients are known and can be used here. Such emollients include, but are not limited to; hydrocarbon oils and waxes, silicon oils, oils and fats triglycerides, esters of acetoglycerides, ethoxylated glycerides, alkylesters of fatty acids having from 10 to 20 carbon atoms, alkenyl esters of fatty acids having from 10 to 20 carbon atoms, fatty acids having from 8 to 22 carbon atoms, fatty alcohols having from 8 to 22 carbon atoms, ethers of fatty alcohols, ester-ethers, lanolin and derivatives, polyhydric alcohols and their polyether derivatives, wax esters, beeswax derivatives, vegetable waxes, phospholipids, sterols, and amides . SAGARIN, COSMETICS, SCIENCE AND TECHNOLOGY, 2nd Edition, Vol. 1, pp. 32-43 (1972) incorporated herein by reference, contains numerous examples of suitable emollient materials. The topical compositions of the invention can be formulated as a cream. Preferably, the creams of the present invention comprise a safe and effective amount of the active sulfohydryl agent; from about 5% to about 50%, preferably from about 10% to about 25% of an emollient; and from about 25% to about 95% water. Optionally, the cream form contains a suitable emulsifier. When an emulsifier is included, it is in the composition at a level of from about 3% to about 50%, preferably from about 5% to about 20%. The emulsifiers can be nonionic, anionic or cationic. Emulsify described is suitable in, for example, the U.S. Patent. No. 3,755,560 published on August 28, 1972, to Dickert and several; the Patent of E.U.A. No. 4,421,769, published December 20, 1983, to Dixon and several: and McCutheon's Deteraents and Emulsifiers. North American Edition, pp. 317-324 (1986); the descriptions of which are incorporated herein by reference. Preferred emulsifiers are anionic and nonionic.

The topical compositions of the invention can also be formulated as a composition comprising a lotion. Preferably the lotions of the invention comprise a safe and effective amount of the sulfohydride active agent; from about 1% to about 50%, preferably from about 3% to about 15% of an emollient; and from about 45% to about 85%, preferably from about 50% to about 75% water. Optionally, the lotion form may contain a suitable emulsifier, ranging from about 3% to about 50%, preferably from about 10% to about 20% of the composition. Examples of suitable emulsifiers are included here above in the description of the cream formulations. Preferably a solution form of the present invention comprises a safe and effective amount of a sulfohydryl active agent, water and a suitable organic solvent. Suitable organic materials useful as solvents or a part of a solvent system are as follows: propylene glycol, glycerin, polyethylene glycol (M. 200-600), polypropylene glycol (MW 425-2025), sorbitol esters, 1,2,6- hexanetriol, ethanol, isopropanol, diethyl tartrate, butanediol, and mixtures thereof. The gel compositions of the present invention can be formulated by simple mixing of a suitable thickening agent to the solution-shaped compositions previously described. The gel compositions preferably comprise a safe and effective amount of the sulfohydride active agent; from about 5% to about 75%, preferably from about 10% to about 50%, of an organic solvent as previously described for the solutions; and from about 0.5% to about 20%, preferably from about 1% to about 10% of a thickening agent. The compositions of solid forms of the present invention have their use as stick-type compositions intended for application to the body. Such compositions preferably comprise a safe and effective amount of the sulfohydride active agent, and from about 50% to about 98%, preferably from about 60% to about 90%, of the previously described emollients. Such compositions may further comprise from about 1% to about 20%, preferably from about 5% to about 15%, of a suitable thickening agent, and optionally emulsifiers and water. Preferred lotions, solutions, sticks, gels and creams, more preferably also contain a preservative, a preservative improver, zinc, and / or zinc salts as described herein. These agents can be incorporated into the aforementioned formulations in the amounts described herein. The compositions of the present invention are preferably formulated to have a pH of 7 or less. The pH values of these compositions preferably range from about 2 to about 7, more preferably from about 3 to about 6, more preferably from about 4.5 to about 5.5. Compositions having a pH within the range of about 4.5 to 7 tend to exhibit less skin irritation, less odor, and greater shelf-storage stability in relation to corresponding compositions having a pH greater than about 8.5.

OTHER INGREDIENTS The compositions of this invention may contain other ingredients, including but not limited to preservatives, improved preservatives, and active agents in addition to the sulfohydride active agent. However, certain agents may decrease the activity of the sulfohydryl compound, particularly N-acetyl-L-cysteine, in topical formulations. First, an excessive number of microbial agents can decrease the activity of the sulfohydryl compound, for example by microbial metabolism of the compound. Second, it has been found that formaldehyde can chemically react with the sulfohydryl compound to decrease its activity. Thus, when a composition containing the sulfohydride compound is formulated with a formaldehyde, or a preservative or other material that forms formaldehyde, the composition may have decreased activity of the sulfohydryl compound over time, relative to the corresponding formulation that does not contain formaldehyde or a compound capable of forming formaldehyde. Therefore, it is desirable to provide compositions containing sulfohydride compounds that have an effective preservative and that does not include formaldehyde or preservatives or other formaldehyde forming material. The compositions are, therefore, preferable and substantially free of formaldehyde and materials that can form or release formaldehyde when present in the composition, including preservatives that can form or release formaldehyde in the composition. The formaldehyde and materials that can form or release formaldehyde in the composition, are alternatively referred to herein as "formaldehyde donor (s)". As used herein, the term "substantially free of formaldehyde donors" means that there are no detectable formaldehyde donors, preferably no formaldehyde donors. The presence of formaldehyde donors may be indicated by the presence of formaldehyde in the composition by any suitable analytical technique, for example high pressure liquid chromatography. The presence of such donors can be initially detected or evidenced by the generation of formaldehyde over time. The topical compositions of the invention preferably comprise one or more preservatives. Preferred preservatives are those that are substantially free of formaldehyde donors. Thus, the preferred preservatives for use herein, are those that do not form or release formaldehyde in the composition either in the preservation process or in an unrelated process. In contrast, conservatives that form or release formaldehyde form or release formaldehyde in the composition either in the preservation process or in an unrelated process. More preferred preservatives include benzyl alcohol, propylparaben, ethylparaben, butylparaben, methylparaben, benzylparaben, isobutylparaben, phenoxyethanol, ethanol, sorbic acid, benzoic acid, methylchloroisothiazolinone, methylisothiazolinone (a preservative containing a mixture of methylchloroisothiazolinone and methylisothiazolinone being commercially available, for example by Rohm & Haas as Kn CGR), methyl dibromoglutarnitrile (commercially available, for example, from Calgon as Tektamer 38R), dehydroacetic acid, o-phenylphenol, sodium bisulfite, dichlorophen, salts of any of the aforementioned compounds, and mixtures of any of the aforementioned compounds. Although the most preferred preservatives are selected from the group consisting of benzyl alcohol, propylparaben, methylparaben, f-enoxyethanol, methylchloroisothiazolinone, methylisothiazolinone, benzoic acid, salts of any of the above preservatives, and mixtures of any of the above compounds. The most preferred preservatives are benzyl alcohol, propylparaben, methylparaben, phenoxyethanol and mixtures thereof. Still, although more preferred, the preservative is a mixture of propylparaben and methylparaben with either or both of benzyl alcohol and phenoxyethanol. In addition to the stability of the sulfohydride compound, these mixtures provide a broad conservative efficacy with nothing or only minimal risk of skin irritation to the user. More preferably, the preservative is a mixture of benzyl alcohol, propylparaben and methylparaben. In addition to the stability of the sulfohydryl compound and the broad conservative efficacy, this mixture presents a particularly low risk of skin irritation to the user. The use of the above preservatives which are substantially free of formaldehyde donors are described in more detail in the co-pending US patent application, entitled "Topical compositions comprising N-acetyl-L-cysteine", filed on June 7, 1995, in the name of Greg C. Hillebrand and Marcia S. Schnicker, which is incorporated herein by reference in its entirety. The above preservatives are preferably used the compositions of the present invention in the same amounts as described for the compositions of the referenced patent application. The compositions of this invention preferably comprise a safe and effective amount of a preservative improver. As used herein, the term "preservative enhancer" means an agent whose purpose is to improve the activity of the conservative. As will be understood by the artisan who has ordinary experience, the conservative improver by itself typically does not provide sufficient efficiency; This tends to increase the effectiveness of the conservative. The improvement of conservative efficacy may involve chelation. Preferred preservative builders useful in the present invention include ethylenediaminetetraacetic acid (EDTA), butylene glycol, propylene glycol, ethanol, and mixtures thereof. Where the preservative includes a paraben, ie, methyl or propylparaben, EDTA is the preferred preservative improver. The use of such enhancers is described in more detail in the above-referenced and incorporated co-pending US patent application, entitled "Topical compositions comprising N-acetyl-L-cysteine", filed on June 7, 1995, in the name of Greg G. Hillebrand and Marcia S. Schnicker. The preservative improvers are preferably used in the compositions of this invention, in the same amounts as described for the compositions of the reference patent application. The compositions of the invention preferably contain zinc or a zinc salt which can be complexed with the sulfohydryl compound. Without being bound by theory, zinc most likely removes the odor by forming a complex with the foul H2S, which can be formed into traces like the decomposed sulfohydride compound. The zinc may additionally or alternatively increase the stability of the sulfohydride compound. The use of zinc salts, in a manner that is suitable for the present invention, is further described in the U.S. patent. No. 5,296,500, Hillebrand, published March 22, 1994, which is incorporated herein by reference. The compositions of the invention may optionally comprise other active agents capable of functioning in different ways to enhance the benefit of the sulfohydryl active agent (thus, the other active agents should not significantly reduce the activity of the sulfohydryl compound). Examples of such substances include, but are not limited to, anti-inflammatory agents, anti-androgens, hair growth suppressants / depilatories, sunscreens, sunscreens, and humectants.

A. Anti-inflammatory. An anti-inflammatory agent can be included as an active agent in the invention, preferably from about 0.1% to about 10%, more preferably from about 0.5% to about 5% of the composition. The exact amount of the anti-inflammatory agent that will be used in the composition will depend on the particular anti-inflammatory agent used, since such agents vary widely in potentiality. Suitable anti-inflammatory agents include steroidal anti-inflammatories, such as hydrocortisone, alpha-methyldexametasone, beclomethasone, dipropionate, and amcinafel; non-steroidal anti-inflammatories, such as oxicams, salicylates, acetic acid derivatives, fenamates, pyrazoles and propionic acid derivatives; also as "natural" anti-inflammatories, such as candelilla wax, alpha bisabolol, aloe vera, Manjistha (extracted from plants of the genus Rubia), and Guggal (extracted from plants of the genus Commiphora).

B. Anti-androgens. In a preferred composition useful in the present invention, an anti-androgen is included as an active agent together with the sulfohydryl active agent. As used herein, the term "anti-androgen" means a compound capable of correcting irregularities in relation to androgens by interfering with the action of androgens on their target organs. The organ object of the present invention is the skin of the mammal. A safe and effective amount of an anti-androgen can be added to the useful compositions of the present invention, preferably from about 0.001% to about 1%, more preferably from about 0. 01% to approximately 0.1%. Anti-androgens that are androgen receptor antagonists as well as anti-androgens that are 5-alpha reductase inhibitors are useful in the compositions of the present invention. Examples of such anti-androgens are more fully described in the U.S. Patent. No. 4,888,336, Holt, Metcalf and Levy, published December 19, 1989; Patent of E.U.A. No. 5,110,939, Holt, Metcalf and Levy, published May 5, 1992; Patent of E.U.A. No. 5,120,742, Rasmusson and Reynolds, published June 9, 1992, and U.S. Pat. No. 4,859,681, Rasmusson and Reynolds, published August 22, 1989; all incorporated here by reference. Also see, M., and P. Pochi, "Anti-androgens and the Skin", International Society of Tropical Dermatolocry. Vol. 17, No. 3, pp 167-179 (1978); incorporated here by reference. Preferred useful anti-androgens in compositions of the present invention are cyproterone acetate, finasteride, chlormadinone acetate, 17-alpha propilmesterolona acetate, 17-alpha estradiol diacetate dienoestrol, estradiol benzoate, inocoterone acetate, spironolactone, 11 -alpha hydroxyprogesterone and cyproterone acetate thioacetate.

C. Hair Growth Suppressants / Depilatories In a preferred composition useful in the present invention, a hair growth or depilator suppressant is included as an active agent together with the sulfohydride active agent. As used herein, the term "depilatory" means an agent capable of removing hair from the skin by breaking the disulfide bonds in the hair keratin, thereby causing the hair fiber to disintegrate. A safe and effective amount of a depilatory agent can be added to the compositions useful in the present invention, preferably from about 0.001% to about 1%, more preferably from about 0.05% to about 0.5%. Preferred depilatories useful in the present invention include tioglicato ammonium, barium sulfate, calcium tioglicato, tioglicato ethanolamine, mercaptopropionic acid, potassium tioglicato, tioglicato sodium, thioglycerol, thioacetic acid tioglícico acid. As used herein, the term "hair growth suppressant" means an agent capable of retarding hair growth. A preferred hair growth suppressant useful in the present invention is diethyldithiocarbamic acid.

D. Solar Filters and Blockers A filter or sunscreen is included as an active agent together with the active agents of the invention in preferred compositions of the present invention. A wide variety of conventional sunscreen agents are suitable for use in combination with exfoliation agents. Segarin and several, in Chapter VIII, pages 189 et seq., Of Cosmetics Science and Technology, describe numerous suitable agents, incorporated herein by reference. Specific suitable sunscreen agents include, for example: p-aminobenzoic acid, its salts and its derivatives (ethyl, isobutyl, glyceryl esters, p-dimethylaminobenzoic acid); anthranylates (e.g. o-aminobenzoates; methyl, menthyl, phenyl, benzyl, phenylethyl, linalyl, terpinyl, and cyclohexenyl esters); salicylates (amyl esters, phenyl, octyl, benzyl, menthyl, glyceryl and dipropylene glycol); cinnamic acid derivatives (benzyl and menthyl esters, a-phenyl cinnamonitrile, butylcinnamoyl pyruvate); dihydroxycinnamic acid derivatives (umbelliferone, methylumbelliferone, methylaceto-umbelliferone); trihydroxycinnamic acid derivatives (esculetin, metilesculetin, dafnetin and the glucosides, esculin and dafinin); hydrocarbons (diphenylbutadiene, stilbene); dibenzalacetone and benzalacetophenone (sodium salts of 2-naphthol-3,6-disulfonic acids and 2-naphthol-6,8-disulfonic acids); dihydroxy-naphthoic acid and its salts; o- and p-hydroxybiphenyldisulfonates; coumarin derivatives (7-hydroxy, 7-methyl, 3-phenyl); diazoles (2-acetyl-3-bromoindazole, methylnaf toxazole, various arylbenzothiazoles); quinine salts (bisulfate, sulfate, chlorine, oleate, and tannate); quinoline derivatives (salts of 8-hydroxyquinoline, 2-phenylquinoline); methoxy or hydroxy substituted benzophenones; uric and vilouric acids; tannic acid and its derivatives (hexaethyl ether); (butylcarbotol) (6-propylpiperonyl) ether; hydroquinone; benzophenones (oxibenzene, sulisobenzone, dioxybenzone, benzoresorcinol, 2, 2 ', 4,4'-tetrahydroxybenzophenone, 2,2'-dihydroxy-4, 4'-dimethoxybenzoone, octabenzone, 4-isopropyldibenzoylmethane, ethocylene; - (4'-methylbenziliden bornan-2-one) and 4-isopropyl-di-benzoylmethane, of which 2-ethylhexyl-p-methoxycinnamate, 4,4'-t-butylmethoxydibenzoylmethane, 2-hydroxy-4-methoxybenzofenone are preferred. , octyldimethyl-p-aminobenzoic acid, digaloyltrioleate, 2,2-dihydroxy-4-methoxybenzophenone, ethyl-4- (bis (hydroxypropyl) -aminobenzoate, 2-ethylhexyl-2-cyano-3,3-diphenylacrylate, 2-ethylhexylsalicylate, glyceryl-p-aminobenzoate, 3,3,5-trimethylcyclohexyl-salicylate, methylanthranilate, p-dimethylaminobenzoic acid or aminobenzoate, 2-ethylhexyl-p-dimethylaminobenzoate, 2-phenylbenzimidazole-5-sulfonic acid, 2 - (p-dimethyl-aminophen enyl) -5-sulphon-benzoxazole and mixtures of these compounds.The most preferred sunscreens useful in the compositions useful in the This invention is 2-ethylhexyl-p-methoxycinnamate, butylmethoxydibenzoylmethane, 2-hydroxy-4-methoxybenzophenone, octyldimethyl-p-aminobenzoic acid and mixtures thereof. Also particularly useful in the compositions are sunscreens such as those described in the U.S. Patent. No. 4,937,370, issued to Sabatelli on June 26, 1990 and the Patent of E.U.A. No. 4,999,186 issued to Sabatelli and Spirnak on March 12, 1991, which are incorporated herein by reference. The sunscreen agents described there have, in a simple molecule, two distinct chromophoric portions that exhibit different absorption spectra of ultra-violet radiation. One of the chromophore portions absorbs predominantly on the UVB radiation scale and the other strongly absorbs on the UVA radiation scale. Preferred members of this class of sunscreen agents are 4-N, N- (ethylhexyl) methylaminobenzoic acid ester of 2,4-dihydroxybenzophenone; N, N-di- (2-ethylhexyl) -4-aminobenzoic acid ester with 4-hydroxydibenzoylmethane; esters of 4-N, N- (2-ethylhexyl) methylaminobenzoic acid with 4-hydroxydibenzoylmethane; 4-N, N- (2-ethylhexyl) methylaminobenzoic acid ester of 2-hydroxy-4- (2-hydroxyethoxy) benzophenone; 4-N, N- (2-ethylhexyl) methylaminobenzoic acid ester of 4- (2-hydroxyethoxy) dibenzoylmethane; N, N-di- (2-ethexyl) -4-aminobenzoic acid ester of 2-hydroxy-4- (2-hydroxyethoxy) benzophenone; and N, N-di- (2-ethylhexyl) -aminobenzoic acid ester of 4- (2-hydroxyethoxy) dibenzoylmethane and mixtures thereof. A safe and effective amount of sunscreen can be used as an additional active agent in the compositions useful in the present invention. The sunscreen agent must be compatible with the active sulfohydride agent. The composition preferably comprises from about 1% to about 20%, more preferably from about 2% to about 10%, of a sunscreen agent. The exact amounts will vary depending on the type of sunscreen chosen and the desired Sun Protection Factor (SPF). An agent can also be added to any of the compositions useful in the present invention to improve the substantivity of the skin of those compositions, particularly to increase their resistance to being removed by water, or removed. A preferred agent that will provide this benefit is a copolymer of ethylene and acrylic acid. Compositions comprising this copolymer are described in the patent of E.U.A. 4,663,157, Brock, published May 5, 1987, which is incorporated herein by reference.

E. Moisturizers In a preferred composition useful in the present invention, a humectant is included as an active agent together with the sulfohydride active agent. Preferred humectants useful in the present invention include glycerol, mineral oil, petrolatum, isopropyl myristate and hyaluronic acid. More preferred humectants include glycerol and petrolatum. The compositions of the present invention are generally prepared by conventional methods, such as are known in the art for making topical compositions. Such methods typically involve mixing the ingredients to a relatively uniform state, with or without heating, cooling, vacuum application, and the like. For optimum stability of the sulfohydride compounds, the compositions of this invention should be manufactured, packaged and stored in a manner that avoids simple air oxidation of the sulfohydride compounds, which is well known in the art. In this way, the exposure of the compositions to air during manufacturing, packaging and storage should be minimized.

Methods of Supplying Topical Compositions Topical compositions useful for the methods of the present invention may be supplied from a variety of delivery devices. The following are two non-limiting examples: A. Medicated cleaning pads The compositions useful herein can be incorporated into a medicated pad. Preferably these alhomadillas comprise from about 50% to about 75% by weight of one or more layers of nonwoven fabric material and from about 20% to about 50% by weight of a liquid composition available from the nonwoven fabric material, preferably comprising from about 0.01% to about 20% active agent, more preferably from about 1% to about 10%, even more preferably from about 2% to about 7%, also preferably 5% active agent. These pads are described in detail in the U.S. Patent. No. 4,891,228, issued to Thaman and several, on January 2, 1990; and the patent of E.U.A. No. 4,891,227, issued to Thaman and several, on January 2, 1990; which are incorporated by reference.

B. Delivery Devices The compositions useful herein may also be incorporated into and supplied from a soft nozzle or flexible delivery device. These devices are useful for the controlled delivery of the compositions to the surface of the skin and have the advantage that the treatment composition itself never needs to be handled by the users. Non-limiting examples of these devices comprise a fluid container that includes a mouth, an applicator, means for handling the applicator in the mouth of the container, and a valve that responds to the normally closed pressure to allow fluid flow from the container to the applicator when the application of pressure to the valve occurs. The valve may include a diaphragm formed of a fluid impervious material with a plurality of arcuate non-intersecting slits therein, wherein each slit has a base that is intersected by at least one other slit, and where each slit is outside the slit. intersecting relationship with its own base, and where there are means to arrange the valve in the container inside the applicator. Examples of these applicator devices are described in the U.S. Patent. No. 4,693,623, to Schwartzman, published September 15, 1987; in the U.S. Patent. No. 4,620,648, Schwartzman, published September 15, 1987; in the U.S. Patent. No. 3,669,323, Harker et al., Published June 13, 1972; in the U.S. Patent. No. 3,418,066, by Schwartzman, published December 24, 1968; and in the U.S. Patent. No. 3,410,645, by Schwartzman, published on November 12, 1968; all of which are incorporated here by reference. Examples of applicators useful herein are commercially available from Dab-O-Matic, Mount Vernon, NY.

M $ tQdog dt? The compositions of the present invention are useful in the removal of unwanted hair, and / or regulation of hair growth, and / or softening of terminal hair. A preferred method of applying the compositions of the present invention involves multiple topical applications to the face, armpits, legs and other areas where unwanted hair is likely to grow. Once applied, the composition is left. The amount of the composition and the frequency of application can vary widely, depending on the area in question, the desired effect and / or personal needs, but it is suggested as an example that topical application preferably varies from approximately five times daily, to one every other day, more preferably from about 3 times a day to once a day, and more preferably about twice a day. The composition for topical application will preferably contain from about 0.001 to about 50 mg of the active agent per cm2 of skin receiving the topical composition, more preferably from about 0.01 to about 30 mg / cm2, more preferably still from about 0.05 to about 10 mg / cm2, also preferably from about 0.1 to about 2mg / cmz. The period of topical application should be as needed by the individual, and may be on the life of the adult subject, for continuous regulation of hair growth and / or removal of unwanted hair.

EXAMPLES The embodiments of the composition of the present invention are illustrated in the following non-limiting examples. All parts, percentages and proportions used here are by weight, unless otherwise specified.

Example I A topical composition was prepared by combining the following components, using conventional mixing techniques and the pH was adjusted to 6.0 by the addition of NaOH Component% by weight N-acetyl-L-cysteine 5. 0 Propylene glycol 45 0 Ethanol 30 .0 Water 20. 0 The lOOOmg of the composition was applied topically to the face by lOOcrn2 of skin, twice a day, to remove unwanted hair.

Example II A topical composition was prepared by combining the following components, using conventional mixing techniques and the pH was adjusted to 4.5 by the addition of NaOH. Component% by weight Thioglycolic acid 2.0 Propylene glycol 57.0 Ethanol 20.0 Water 10.0 Benzyl alcohol 4.0 Glycerin 5.0 Miristilic alcohol 2.0 4000mg of the composition per lOOcm2 of skin is applied topically once a day to the legs to soften the terminal hair.

EXAMPLE III A topical composition was prepared by combining the following components, using conventional mixing techniques and the pH was adjusted to 3 by the addition of NaOH.

Component% by weight Glutathione 1. 0 Propylene glycol 30 0 Glycerin 3 0 Water 66. 0 It was applied topically to the face 2000mg of the composition for lOOcm2 of skin, twice a day, to remove unwanted hair.

EXAMPLE IV A topical composition was prepared by combining the following components, using conventional mixing techniques and the pH was adjusted to 5 by the addition of NaOH. Component% by weight N-acetyl-L-cysteine 0.5 Propylene glycol 30.0 Propylene glycol laureth 1.0 Isopropanol 20.0 Water 48.5 500mg of the composition was applied topically to the face for 10OOcm2 of skin, once a day, to remove unwanted hair.

Example V A lotion was prepared by combining the following components, using conventional mixing techniques and the pH was adjusted to 4 by the addition of NaOH. Component% by weight Cysteine 5.0 Cetyltrimethylammonium chloride 4.0 diparcially hydrogenated tallow 2.0 Cetyltrimethylammonium chloride DC-200 fluid (12500 csk) * 1.0 Citric acid 3.5 Ethylene glycol distearate 1.5 PEG-3 C12 alkylamide 3.0 Water 80.0 * Dimethylpolysiloxane available from Dow Chemical Co.

Top 100 mg of the composition was applied topically to the face by lOOcm2 of skin, three times a day, to remove unwanted hair.

Examples VI-VIII Lotions, containing the following compositions, were prepared using conventional mixing techniques and the pH was adjusted to 4.5 by the addition of NaOH.

Example NO ,. VI VII VIII Component% by weight% _ by weight% weight N-acetylcysteine 0.1 0.5 2.0 Hydroxyethylcellulose 0.4 0.4 Absolute ethanol 15.0 15.0 15.0 Propane- 1,2-diol 30.6 Butane- 1, 3-diol 33.4 33.4 Paramethylbenzoate 0.2 0.2 0.2 Perfume 0.5 0.5 0.5 Water 50.4 50.4 48.7 The use of an amount of any of the above compositions to deposit approximately 750 mg per 10000 cm of the composition to the armpit area, once a day, is appropriate after the initial shave removal. The replaced hair is softer than the hair removed.

Example IX An oil-in-water emulsion was prepared by combining the following ingredients, using conventional mixing techniques and the pH was adjusted to 6.5 by the addition of NaOH. Component% by weight Oily phase Lipoic acid 5.0 Cetearyl alcohol 5.0 Silicon oil, 200 fluid 5.0 Isopropylamistate 2.0 Sodium stearoyl-2-lactylate 2.0 Aqueous phase Propylene glycol 5.0 Sodium citrate 0.2 Perfume 0.1 Water 79.7 The emulsion was prepared by taking 10 parts of the oily phase and adding it slowly with stirring to 90 parts by volume of the aqueous phase. The use of an amount of the emulsion to deposit approximately lOOOmg per lOOcm2 of the emulsion, three times a day to the legs is appropriate, after the initial hair is shaved off. The terminal hair replaced is softer than the hair removed.

Example X An oil-in-water cream was prepared by mixing the following components and the pH was adjusted to 3.5 by the addition of NaOH. Component% by weight Oily phase N-acetyl-L-cysteine 5.0 Sorbitan monoleate 20.0 Quaternium-18-hectonite 5.0 Liquid paraffin 60.0 Aqueous phase Xanthan gum 1.0 Conservative 0.3 Perfume 0.2 Water 8.5 The cream was prepared by mixing the oily phase and heating to 65 ° C. The aqueous phase was combined and heated to 70 ° C. The aqueous phase was added to the oil phase with suitable agitation. Moderate agitation was applied while cooling. Approximately 5mg of the cream was placed per lOOcm2 on the face, once a day, to remove unwanted hair.

Example XI An oil cream in water is prepared by mixing the following components and adjusting the pH to 4.5. The cream is prepared as described in Example X. Component% by weight Oil phase Perfume 0.20 Cetyl alcohol, NF 1. 00 Stearic alcohol, NF 1.00 Polyoxyethylene (50:50 -12/20) 1.00 cetyl / stearyl ( 50:50) Dicaprilato / Dicaprate of 3.00 propylene glycol Monostearate of glycerol 2.00 Palmitate-monostearate of 2.00 glyceryl Phase Aqueous N-acetyl-L-cysteine 5.25 Distilled water 77.19 Glycerin 3.00 Citric acid 0.50 Benzyl alcohol 0.50 Propylparaben 0.1 Methylparaben, NF 0.25 Oxide of zinc, USP 0.26 Butylene glycol 1.50 Sodium Hydroxide 1.12 Disodium EDTA 0.13 Approximately 5mg of the cream was placed per lOOcm2 on the face, once a day, to remove unwanted hair. The cream exhibits increased shelf-storage stability, particularly of N-acetyl-L-cysteine, in relation to a corresponding composition containing a formaldehyde donor, such as a preservative that forms or releases formaldehyde in the composition as part of the preservation. or another process. In this way, the cream exhibits increased N-acetyl-L-cysteine efficacy, in relation to the same corresponding composition. While particular embodiments of the present invention have been described, it will be obvious to those skilled in the art, that various changes and modifications of the present invention may be made without departing from the spirit and scope of the invention. In the appended claims, it is intended to protect all those modifications that are within the scope of the invention.

Claims (6)

1. NEWS OF THEINVENTION CLAIMS 1. A topical depilatory composition, characterized in that the composition comprises: a) a safe and effective amount, preferably from 0.1% to 15%, more preferably from 0.5% to 10%, but more preferably from 1% to 7%, most preferably from 2% to 5%, of a sulfohydryl compound selected from the group consisting of: thioglycolic acid, cysteine, homocysteine, glutathione, thioglycerol, thiomalic acid, 2-mercaptopropionic acid, 3-mercaptopropionic acid, thiodiglycol, 2-mercaptoethanol, dithiothreitol, thioxanthane, thiosalicylic acid, thiolactic acid, thiopropionic acid, thiodiglycolic acid, N-acetyl-L-cysteine, lipoic acid, and cosmetically and / or pharmaceutically acceptable salts thereof; preferably thioglycolic acid, cysteine, glutathione, N-acetyl-L-cysteine, lipoic acid, thiosalicylic acid, thiolactic acid and cosmetically and / or pharmaceutically acceptable salts thereof; more preferably thioglycolic acid, cysteine, glutathione, N-acetyl-L-cysteine, and cosmetically and / or pharmaceutically acceptable salts thereof; the most preferable are N-acetyl-L-cysteine and a cosmetically and / or pharmaceutically acceptable salt thereof; and b) a safe and effective amount of a topical vehicle, such that the composition has a pH of 7 or less, preferably 3 to 6, more preferably 4.5 to 5. 5. The topical depilatory composition, according to claim 1, further characterized in that said topical vehicle comprises an emollient. 3. The topical depilatory composition according to claim 1 or 2, further characterized in that said composition further comprises a hair growth suppressant. 4. A method for removing unwanted hair in mammals, characterized in that the method comprises topically applying to a mammal in need of treatment, preferably five times a day to once every two days, more preferably three times a day at a time per day, a composition comprising: a) a safe and effective amount of a sulfohydryl compound selected from the group consisting of thioglycolic acid, cysteine, homocysteine, glutathione, thioglycerol, thiomalic acid, 2-mercaptopropionic acid, 3-mercaptopropionic acid, thiodiglycol, 2-mercaptoethanol, dithiothreitol, thioxanthane, thiosalicylic acid, thiolactic acid, thiopropionic acid, thiodiglycolic acid, N-acetyl-L-cysteine, lipoic acid, and cosmetically and / or pharmaceutically acceptable salts thereof; preferably thioglycolic acid, cysteine, glutathione, N-acetyl-L-cysteine, lipoic acid, thiosalicylic acid, thiolactic acid and cosmetically and / or pharmaceutically acceptable salts thereof; more preferably N-acetyl-L-cysteine and a cosmetically and / or pharmaceutically acceptable salt thereof; and b) a safe and effective amount of a topical vehicle, such that the composition has a pH of 7 or less, preferably from 3 to 6; the amount of said sulfohydride compound applied to the skin preferably being O.Olmg per cm2 of skin at 30mg per cm2, more preferably O.OSmg per cm2 of skin at 10mg per cm2 of skin. A method for smoothing terminal hair on the skin of a mammal, characterized in that the method comprises topically applying to a mammal in need of treatment a composition comprising: a) a safe and effective amount of a sulfohydryl compound selected from the group which consists of thioglycolic acid, cysteine, homocysteine, glutathione, thioglycerol, thiomalic acid, 2-mercaptopropionic acid, 3-mer cap topropionic acid, thiodiglycol, 2-mercaptoe anol, dithiothreitol, thioxanthane, thiosalicylic acid, thiolactic acid, thiopropionic acid, thiodiglycolic acid, N-acetyl-L-cysteine, lipoic acid, and cosmetically and / or pharmaceutically acceptable salts thereof; preferably N-acetyl-L-cysteine and a cosmetically and / or pharmaceutically acceptable salt thereof; and b) a safe and effective amount of a topical vehicle, such that the composition has a pH of 7 or less, preferably from 3 to 6; IN WITNESS WHEREOVER, I sign the above in this City of Mexico, D.F., on the 9th day of the month of February of 1996. By THE PROCTER & GAMBLE COMPANY Liliana Hernández Suárez DEPILATORY COMPOSITIONS COMPRISING SULFOFFlDRILO COMPOUNDS EXTRACT OF THE INVENTION The present invention involves topical depilatory compositions, at a pH of 7 or less, comprising sulfohydride compounds. The present invention further relates to methods for removing fur from mammalian skin, comprising the topical application of a composition, at a pH of 7 or less, comprising a sulfohydryl compound or a cosmetically and / or pharmaceutically acceptable salt thereof. .