JPH09509933A - Anti-acne composition - Google Patents

Abstract

  (57) [Summary] The present invention relates to anti-acne compositions comprising a combination of benzoyl peroxide and a zwitterionic surfactant. The invention further relates to a method of treating acne on mammalian skin.

Description

DETAILED DESCRIPTION OF THE INVENTION Anti-acne composition Technical Field The present invention relates to the field of treatment acne in mammalian skin. Specifically, the invention relates to a method of treating acne in human skin. BACKGROUND OF THE INVENTION Acne is a pilosebaceous disease characterized by comedones, papules, inflammatory nodules and surface pus filled cysts. The course and severity of acne is determined by interactions between hormones, keratinization, sebum formation and bacteria. Acne usually begins during puberty, when the pilosebaceous gland enlarges, and sebum synthesis activity increases due to increased circulating levels of androgens. Vesicle hyperkeratosis also occurs, compressing the pilosebaceous follicles and thus forming a comedone or plug. Comedones contain sebum, protein residues, and anaerobic microorganisms including Propionibacterium [Corynebacterium] acnes (P. acnes). P. Acnes propagates in sebum to form inflammatory free fatty acids (FFA). FFA stimulates the vesicle wall, destroys it and induces inflammatory lesions. In severe cases, the lesion heals even after it heals. Current treatments for acne include general topical application of lotions and ointments to the affected skin surface, as well as localized topical treatment. The products used in such treatments contain antimicrobial agents such as benzoyl peroxide. The object of the present invention is to provide a topical composition for the treatment of acne on mammalian skin. Another object of the present invention is to destroy the vesicle plugs to prevent the presence of P. It is to provide such a composition capable of delivering more benzoyl peroxide to Acnes than current compositions. Another object of the present invention is to provide a method for treating acne in mammalian skin. Another object of the invention is to enhance the delivery of benzoyl peroxide by P. It is an object of the present invention to provide a method for treating acne in mammalian skin, which controls acnes proliferation. SUMMARY OF THE INVENTION The present invention relates to the combination of benzoyl peroxide with certain dipolar surfactants having the structure: In the above formula, (a) R ¹ is an unsubstituted, saturated or unsaturated, straight chain or branched chain alkyl having about 9 to about 22 carbon atoms; (b) m is an integer of 1 to 3; c) n is 0 or 1; (d) R ² and R ³ are independently saturated straight chain alkyl having 1 to about 3 carbon atoms which is unsubstituted or monosubstituted by hydroxy. (E) R ⁴ is a saturated or unsaturated, straight or branched chain alkyl having 1 to about 5 carbon atoms, which is unsubstituted or mono-substituted with hydroxy; and (f) X is CO ₂ , SO ₃ or SO ₄ . The compositions of the present invention include a safe effective amount of a benzoyl peroxide together with a safe effective amount of a dipolar surfactant, and a pharmaceutically acceptable carrier. The present invention also includes methods of using such compositions for the prevention or treatment of acne. These and other features, aspects and advantages of the present invention will become better understood with reference to the following description and appended claims. DETAILED DESCRIPTION OF THE INVENTION The combination of benzoyl peroxide and certain zwitterionic surfactants has been found to be unexpectedly useful in the treatment of acne. Without being limited to any particular mechanism, it is believed that the composition exhibits the ability to destroy vesicle plugs in mammalian comedones. This combination is thought to work by affecting the proteolytic enzymes on the skin surface that disrupt the protein junctions (desmosomes) between cells at the vesicle plug, thus causing cell or scale detachment. As used herein, "desquamation" refers to exfoliation or removal of scale from the outermost layer (stratum corneum) of the epidermis. Exfoliation is thought to be useful in the treatment of acne, as it breaks the comedone on the skin with acne. As used herein, “treating acne” means preventing, delaying and / or preventing the process of acne formation in mammalian skin. The term "alkyl", as used herein, unless otherwise indicated, is straight or branched, substituted or unsubstituted, saturated, monounsaturated (ie one double or triple bond in the carbon chain). Or a carbon-containing chain which is polyunsaturated (that is, two or more double bonds in the carbon chain, two or more triple bonds in the carbon chain, one or more double and one or more triple bonds in the carbon chain). The preferred alkyl is straight chain. Preferred alkyls are mono- or di-substituted or unsubstituted, more preferably unsubstituted. Preferred alkyls are saturated or monounsaturated, if so preferably double bonds, more preferably alkyls are saturated. Preferred alkyl substituents include halogen, aryl, amino, hydroxy, alkoxy, cyano, nitro and trifluoromethyl. More preferred alkyl substituents are halogen and aryl. "Zipolar surfactant" as used in the present invention means a compound having the following structure: In Structure (I), R ¹ is unsubstituted alkyl having about 9 to about 22 carbon atoms. Preferred R ¹ has about 11 to about 18 carbon atoms, more preferably about 12 to about 16 carbon atoms, and even more preferably about 14 to about 16 carbon atoms. In the structure (I), m is an integer of 1 to 3, preferably 2 or 3, more preferably 3; in the structure (I), n is 0 or 1, and n is preferably 1. In Structure (I), R ² and R ³ are independently selected from the group consisting of saturated straight chain alkyl having 1 to about 3 carbon atoms which is unsubstituted or mono-substituted with hydroxy. Preferred R ² and R ³ are CH ₃ , CH ₂ CH ₂ OH and CH ₂ CH ₂ CH ₂ OH. More preferred R ² and R ³ are CH ₃ . In structure (I), X is selected from the group consisting of CO ₂ , SO ₃ and SO ₄ . In Structure (I), R ⁴ is an alkyl having 1 to about 5 carbon atoms, unsubstituted or mono-substituted with hydroxy. When X is CO ₂ , R ⁴ preferably has 1 or 3 carbon atoms, more preferably 1 carbon atom. When X is SO ₃ or SO ₄ , R ⁴ preferably has from about 2 to about 4 carbon atoms, more preferably 3 carbon atoms. Preferred dipolar surfactants of the present invention include the following compounds: a) Cetyl betaine: b) cocoamidopropyl betaine: (Wherein R is an unsubstituted, saturated, straight chain alkyl of about 9 to about 13 carbon atoms) c) Cetylpropyl hydroxysultaine: d) Cocoamidopropyl hydroxysultaine: (Wherein R is an unsubstituted, saturated, straight chain alkyl of about 9 to about 13 carbon atoms); and e) behenyl betaine: Further preferred zwitterionic surfactants of the present invention include cetyl betaine, cocoamidopropyl betaine and cetyl propyl hydroxysultaine. Even more preferred zwitterionic surfactants of the present invention include cetyl betaine and cetyl propyl hydroxysultaine. The most preferred zwitterionic surfactant of the present invention is cetyl betaine. As used herein, "topical application" means direct application or application to external skin. As used herein, "safely effective amount" means an amount of the composition that is sufficient to induce significant improvement in the condition being treated, but low enough to avoid serious side effects. As used herein, "comprising" means that other steps and ingredients that do not affect the end result can be added. This term encompasses the terms “consisting of” and “consisting essentially of”. As used herein, the term "pharmaceutically acceptable" means that the drug, drug or inactive ingredient represented by the term is used in human without excessive toxicity, incompatibility, instability, irritation, allergic reaction, etc. And below and suitable for use in contact with animal tissue. As used herein, "active agent" means a combination of benzoyl peroxide and a dipolar surfactant according to structure (I) or a mixture of such surfactants. Compositions useful in treating acne preferably contain about 0.1 to about 10%, more preferably about 1 to about 6%, and even more preferably about 2 to about 5% benzoyl peroxide. Compositions useful in treating acne are preferably from about 0.1 to about 10%, more preferably from about 1 to about 6%, and even more preferably from about 2 to about 5% dipolar by structure (I). It also includes a surfactant or a pharmaceutically acceptable salt thereof. Preferred pharmaceutically acceptable salts include alkali metal salts such as sodium and potassium; alkaline earth metal salts such as calcium and magnesium; non-toxic heavy metal salts; ammonium salts; trialkyls such as trimethylammonium and triethylammonium. There is an ammonium salt. Pharmaceutically Acceptable Carriers In addition to the active agent, the pharmaceutical compositions of the present invention essentially include a pharmaceutically acceptable carrier. The term "pharmaceutically acceptable carrier", as used herein, means one or more compatible solid or liquid filler diluents suitable for administration to humans or lower animals. As used herein, the term "compatible" means that the components of the pharmaceutical composition are compounds of the invention such that under normal conditions of use there is no interaction which would substantially reduce the pharmaceutical efficacy of the pharmaceutical composition. And and can be mixed with each other. Pharmaceutically acceptable carriers must, of course, be sufficiently pure and sufficiently low in toxicity to render them suitable for administration to the human or lower animal to be treated. The composition of the invention is administered topically to the biological subject, ie by direct application or application of the composition onto the skin of the subject. Topical compositions useful in the present invention include pharmaceutically acceptable and pharmaceutically acceptable amounts of a composition suitable for topical application to mammalian skin, an active agent as described below or a mixture of such active agents. And a topical carrier. Topical compositions useful in the present invention may be of various product types. These include, but are not limited to, lotions, creams, gels, sticks, sprays, ointments, pastes, mousses and cosmetics. These product types include several types of carrier systems including, but not limited to, solutions, emulsions, gels, solids and liposomes. Topical compositions useful in the present invention formulated as solutions typically contain a pharmaceutically acceptable aqueous or organic solvent. The term "pharmaceutically acceptable organic solvent" relates to a solvent in which an active agent is dispersed or dissolved and which can still have acceptable safety (eg irritation and sensitization). Water is the preferred solvent. Examples of suitable organic solvents are propylene glycol, polyethylene glycol (200-600), polypropylene glycol (425-2025), glycerol, 1,2,4-butanetriol, sorbitol ester, 1,2,6-hexanetriol. , Ethanol, isopropanol, sorbitol ester, butanediol and mixtures thereof. These solutions useful in the present invention preferably contain from about 80 to about 99.99% acceptable aqueous or organic solvent. If the topical composition useful in the present invention is formulated as an aerosol and applied to the skin as a spray on, a propellant is added to the solution composition. Examples are chlorofluorinated low molecular weight hydrocarbons. A more detailed disclosure of propellants useful in the present invention can be found in Sagarin, Cosmetics Science and Technology, 2nd Edition, Vol. 2, pp. 44 3-465 (1972). The topical compositions useful in the present invention may be formulated as a solution containing an emollient. Such compositions preferably contain from about 2 to about 50% of a topical pharmaceutically acceptable emollient. As used herein, "emollient" refers to a substance used to prevent or reduce drying and to protect the skin. Various suitable emollients are known and may be used in the present invention. Sagarin, Cosmetics Science and Technology, 2nd Edition, Vol. 1, pp. 32-43 (1972), incorporated herein by reference, includes many examples of suitable materials. Lotions can also be prepared from solution carrier systems. Lotions typically contain about 1 to about 20%, preferably about 5 to about 10% emollient and about 50 to about 90%, preferably about 60 to about 80% water. Another type of product that may be formulated from a solution carrier system is a cream. Creams typically contain about 5 to about 50%, preferably about 10 to about 20% emollient and about 45 to about 85%, preferably about 50 to about 75% water. Yet another type of product that may be formulated from a solution carrier system is an ointment. Ointments may contain a simple base of animal or vegetable oils or semisolid hydrocarbons (oily). Ointments may also contain an absorbent ointment base which absorbs water to form an emulsion. Ointment carriers may be water-soluble. Ointments may contain from about 2 to about 10% emollient and from about 0.1 to about 2% thickener. A more detailed disclosure of thickeners useful in the present invention can be found in Sagarin, Cosmetics Science and Technology, 2nd Edition, Vol. 1, pp. 72-73 (1972). If the carrier is formulated as an emulsion, preferably about 1 to about 10%, more preferably about 2 to about 5% of the carrier system is an emulsifier. Emulsifiers are nonionic, anionic or cationic. Suitable emulsifiers are, for example, Dickert et al. U.S. Pat. No. 3,755,560 issued Aug. 28, 1973; Dixon et al. U.S. Pat. No. 4,421,769 issued Dec. 20, 1983. And McCutcheon's Detergents and Emulsifiers, North American Edition, pages 317-324 (1986). Cleaning compositions useful in the present invention preferably contain from about 1 to about 90%, more preferably from about 5 to about 10% cosmetically acceptable surfactant. The physical form of the cleansing composition is not critical. The composition can be formulated, for example, as a solid cosmetic, liquid, shampoo, paste or mousse. Solid cosmetics are most preferred because this is the form of cleansing agent most commonly used to cleanse the skin. Rinse off cleansing compositions such as shampoos require a delivery system suitable for providing sufficient levels of active agent on the skin and scalp. Preferred delivery systems use insoluble complexes. For a more detailed disclosure, see Barford et al., US Pat. No. 4,835,148, issued May 30, 1989, which is hereby incorporated by reference in its entirety. The cleaning compositions useful in the present invention can optionally contain materials commonly used in cleansing compositions at their industry established levels. Non-limiting examples of possible surfactants are Isocetes-20, sodium methyl cocoyl taurate, sodium methyl oleoyl taurate and sodium lauryl sulphate. See Kowcz et al., US Pat. No. 4,800,197, issued Jan. 24, 1989, which is hereby incorporated by reference in its entirety. Examples of various additional surfactants useful in the present invention are described in McCutcheon's Detergents and Emulsifiers, North American Edition (1986), Allured Publishing Corporation, incorporated herein by reference in its entirety. . Combination activator A. Anti-inflammatory agent An anti-inflammatory agent may also be included as an active agent together with said active agent to reduce redness and irritation of inflammatory acne lesions. A safe and effective amount of anti-inflammatory agent, preferably about 0.1 to about 10% of the composition, more preferably about 0.5 to about 5%, is added to the compositions useful in the invention. The exact amount of anti-inflammatory agent used in the composition will depend on the particular anti-inflammatory agent utilized, as such agents will vary widely in potency. Although not limited, hydrocortisone, hydroxyltriamcinolone, α-methyldexamethasone, dexamethasone phosphate, beclomethasone dipropionate, clobetasol valerate, desonide, desoxymethasone, desoxycorticosterone acetate, dexamethasone, dichlorisone, diflorazone diacetate, Diflucortron valerate, fluadrenolone, fluchlorolone acetonide, fludrocortisone, flumethasone pivalate, fluocinolone acetonide, fluocinonide, flucortin butyl ester, fluocortron, fluprednidene acetate (flupredenylidene), fluland Lenolone, halcinonide, hydrocortisone acetate, hydrocortisone butyrate, methylprednisolone, triamcinolone acetonide, cortisone, colt Quixone, Flucetonide, Fludrocortisone, Difluorozone diacetate, Fluradrenolone, Fludrocortisone, Diflurozone diacetate, Fluradrenolone acetonide, Medrisone, Amsinafel, Amcinafide, Betamethasone and its esters, Chloprednisone, Chlorprednisone acetate, Clocorterone, Cresinolone , Dichlorisone, diflupredonate, fluchlornide, flunizolide, fluoromethalone, fluperolone, fluprednisolone, hydrocortisone valerate, hydrocortisone cyclopentylpropionate, hydrocortamate, meprednisone, paramethasone, prednisolone, prednisone, beclomethasone dipropionate and triam Including corticosteroids such as a mixture of De antiinflammatory agents may be used. A preferred steroidal anti-inflammatory for use is hydrocortisone. A second class of anti-inflammatory agents useful in the compositions include non-steroidal anti-inflammatory agents. The various compounds included in this group are well known to those skilled in the art. For detailed disclosure of the chemical structure, synthesis, side effects, etc. of non-steroidal anti-inflammatory drugs, see Anti-inflammatory and Anti-Rheumatic Drugs, KD Rainsford, Vol.I-III, CRCPress, Boca Raton (1985) and Anti-inflammatory. Reference is made to standard texts including Agents, Chemistry and Pharmacolgy, 1, RA Scherrer et al., Academic Press, New York (1974). Specific non-steroidal anti-inflammatory agents useful in the compositions of the present invention include, but are not limited to: 1) oxicams such as piroxicam, isoxicam, tenoxicam, sudoxicam and CP-1 4,304; 2). Acetic acid derivatives such as diclofenac, fenclofenac, indomethacin, sulindac, tolmethine, isoxepak, flofenac, tiopinac, zidomethacin, asematacin, fentiazac, zomepirac, clindanac, oxepinac, felbinac and ketorolac; 3) mefenamic acid, fluclofenac acid, meclofenac acid Phenamates such as acids, niflumic acid and tolfenamic acid; 4) ibuprofen, naproxen, benoxaprofen, flurbiprofen, ketoprofen, pheno Propionic acid derivatives such as lofen, fenbufen, indoprofen, indolprofen, carprofen, oxaprozin, pranoprofen, miloprofen, thioxaprofen, spprofen, aluminoprofen and thiaprofenic; and 5) phenylbutazone, oxyphene Pyrazoles such as butazone, feprazone, azapropazone and trimetasone. Mixtures of these non-steroidal anti-inflammatory agents and pharmaceutically acceptable salts and esters of these agents may also be used. For example, the flufenamic acid derivative etofenamate is particularly useful for topical application. Among the non-steroidal anti-inflammatory agents, ibuprofen, naproxen, flufenamic acid, mefenamic acid, meclofenamic acid, piroxicam and felbinac are preferred, and ibuprofen, naproxen and flufenamic acid are most preferred. Finally, so-called "natural" anti-inflammatory agents are also useful in the method of the present invention. For example, candelilla wax, α-bisabolol, aloe vera, Manjistha [extracted from plants of the genus Rubia, in particular Rubia Cordifolia] and Guggal [genus Comiphora, especially Commiphora Mukul]. It is extracted from the plant of.] Is used. B. Retinoids In a preferred composition useful in the present invention, a retinoid, preferably retinoic acid, is included as an active agent together with said active agent. Inclusion of retinoid increases the anti-acne effect of the composition and suppresses sebum production in the skin. A safe and effective amount of retinoid, preferably from about 0.01 to about 0.5% of the composition, more preferably from about 0.01 to about 0.1%, is added to the compositions useful in the invention. As used in the present invention, "retinoid" includes all natural and / or synthetic analogs of vitamin A or retinol-like compounds having the biological activity of vitamin A in the skin, as well as geometric and stereoisomers of these compounds, for example all. Includes trans-retinoic acid and 13-cis-retinoic acid. C. Anti-Androgen Agents In a preferred composition useful in the present invention, an anti-androgen agent is included as an active agent with the active agent. As used herein, "anti-androgen" refers to a compound that can ameliorate an androgen-related disorder by preventing the action of androgens in their target organs. The target organ of the present invention is mammalian skin. Preferred antiandrogens include cyproterone thiopivalate and cyproterone acetate thioacetate. D. Glycolic Acid In a preferred composition of the invention, glycolic acid is included as the active agent with the anti-acne agent. Preferably, the composition comprises about 0.1 to about 10% glycolic acid, more preferably about 1 to about 6%, and even more preferably about 2 to about 5%. E. FIG. Anti-Acne Agents In a preferred composition of the invention, an additional anti-acne agent is included as an active agent with the anti-acne agent. Preferred additional anti-acne agents include hesperetin and phloretin. Preferably, the composition comprises about 0.1 to about 5%, more preferably about 0.5 to about 3%, and even more preferably about 1 to about 2% anti-acne agent. The topical compositions useful in the method of the delivery method of the present invention the topical composition can be delivered from a variety of delivery devices. The following are two non-limiting examples. Medicinal Cleansing Pad The compositions useful in the present invention can be incorporated into a medicated cleansing pad. Preferably, these pads comprise one or more layers of non-woven material comprising about 50 to about 75% by weight of non-woven material and a hydroxy acid including salicylic acid and the present dipolar surfactant or a mixture of such surfactants. From about 20 to about 50% by weight of a liquid composition deliverable from These pads are disclosed in U.S. Pat. No. 4,891,228 to Thaman et al. Issued on Jan. 2, 1990 and U.S. Pat. No. 4,891,227 to Thaman et al. Issued on Jan. 2, 1990. And both of which are incorporated herein by reference in their entirety. Dispensing Device The compositions useful in the present invention can also be delivered in from a soft tipted or flexible dispensing device. These devices are useful for controlled delivery of the composition to the skin surface and have the advantage that the therapeutic composition itself need not be handled directly by the user. Non-limiting examples of these devices include a fluid container having an opening, an applicator, a means for holding the applicator in the opening of the container, and a normally closed pressure sensing valve that allows fluid to flow from the container to the applicator upon pressurization of the valve. Consists of. The fluid consists of a hydroxy acid, including salicylic acid, and the present dipolar surfactant or mixture of such surfactants. The valve may include a diaphragm formed of an elastic fluid impermeable material having a number of non-intersecting arcuate slits therein, each slit having a base that intersects at least one other slit. , Each slit is not in a cross relationship with its own base, and there is a means to attach the valve to the container inside the applicator. Examples of these applicator devices are Schwartzman U.S. Pat. No. 4,693,623 issued Sep. 15, 1987; Schwartzman U.S. Pat. No. 4,620,648 issued Sep. 15, 1987. Harker et al., U.S. Pat. No. 3,669,323, issued June 13, 1972; Schwartzman, U.S. Pat. No. 3,418,055, issued Dec. 24, 1968; Nov. 1968; It is described in Schwartzman's U.S. Pat. No. 3,410,645, issued on Dec. 12, all of which are hereby incorporated by reference in their entirety. Examples of applicators useful in the present invention are commercially available from Dab-O-Matic, Mount Vernon, NY. Therapeutic Methods This invention Acne relates to a method of treating acne in mammalian skin. In such a method, an effective amount of a composition of the present invention is applied topically to the skin or scalp. The term "effective amount" as used herein means an amount sufficient to provide an anti-acne effect. The composition should have suitable intervals until a satisfactory anti-acne effect is obtained: about 3 times / day to about 1 time / 3 days, preferably about 2 times / day to about 1 time / 2 days, and more preferably It can be applied about once a day for several days, weekly, monthly or yearly. Typically, for each application, an effective coating of the skin or scalp will contain from about 0.004 to about 0.1 mg of benzoyl peroxide and the present dipolar surfactant or a mixture of such surfactants, respectively. cm ^2, obtained by even more preferably from about 0.02 to about 0.06 mg / cm ^2, yet which is preferably applied from about 0.04 mg / cm ^2. Examples The following examples further describe and explain embodiments within the scope of the present invention. The examples are provided for illustrative purposes only, and are not to be construed as limitations on the invention, many variations thereof being possible without departing from the spirit and scope of the invention. Example I A topical composition is prepared by admixing the following ingredients utilizing conventional mixing techniques. Ingredient Weight% Water 50.67 Triethanolamine 0.66 Cetylbetaine 6.66 Disodium EDTA 0.01 Ethanol (95%) 32.00 Benzoyl peroxide 10.00 The above composition has a composition of ² mg per cm ^{2 of} skin. Apply once daily to the face to treat acne, in a dose sufficient to lighten. When acne present is gone, application is reduced to once every two days. Example II A cleaning composition is prepared by mixing the following ingredients using conventional mixing techniques. Ingredients Weight% Water 44.75 EDTA tetrasodium 0.12 Cetyl betaine 3.33 Sodium methyl cocoyl taurate 41.67 Cetyl propyl hydroxysultaine 6.00 Benzoyl peroxide 2.00 Coco amido propyl betaine 1.43 Hydroxy propyl methyl cellulose 0.50 Glycolic acid 0.20 Fragrance 0.12 The cleaning composition is applied to the face twice a day to treat acne. An amount sufficient to apply 3 mg of composition per cm ^{2 of} skin is used. Once the acne present is gone, reduce the frequency to once a day. Example III The following topical gel is prepared by mixing the ingredients according to conventional mixing techniques. Ingredients Weight% Alcohol SD-40 (95%) 40.00 Benzoyl peroxide 2.00 Disodium EDTA 0.005 Cetyl betaine 6.66 Water 47.335 Gel is a composition per cm ² skin to treat acne. The product is applied to the face three times daily at a dose of 0.2 mg. As treatment progresses, application is reduced to once a day. Example IV The following lotion is made by mixing the ingredients according to conventional mixing techniques. Ingredient % by weight Water 9.96 Glycerin 10.0 Petrolatum 2.5 Cetyl alcohol 1.8 Cyclomethicone and dimethicone copolyol 1.5 Stearyl alcohol 1.2 Isopropyl palmitate 1.0 Dimethicone 0.5 Sodium hydroxide 0.34 Lanolinic acid 0.25 Polyethylene glycol-100 stearate 0.25 Stearic acid 0.25 Methylparaben 0.2 Titanium dioxide 0.15 EDTA 0.1 Benzoyl peroxide 5.0 Cocoamidopropyl betaine 5.0 The above lotion is skin The composition is applied to the face once a day at a dose of 0.75 mg per cm ² . When the acne present is gone, the frequency of application is reduced to once every two days. Example V The following cleaning solution is prepared by admixing the following ingredients according to conventional mixing techniques. Ingredients Weight% Water 85.3 Carbopol 980 0.9 Cetylbetaine 2.0 EDTA disodium 0.1 NaOH solution (5%) 9.2 Benzoyl peroxide 2.5 The above lotion contains 0 composition per cm ² skin. Apply to face at twice daily dose of 90 mg. When the acne present is gone, the frequency of application is reduced to once a day. Example VI The following lotion is made by mixing the ingredients according to conventional mixing techniques. Ingredient Weight% Carbopol 980 0.9 Water 80.5 EDTA disodium 0.1 Cetyl betaine 2.0 Dow Corning antifoam 1.0 Cetyl alcohol 1.5 Stearyl alcohol 1.5 Steareth-2 ¹ 0.9 Steareth-21 ¹ 0.1 Benzoyl peroxide 2.5 Cyclomethicone D4 / D5 0.5 NaOH solution (5%) 8.5 ¹ Obtained from ICI Americas The above lotion is at a dose of 20 mg of composition per cm ^{2 of} skin. Apply to face once every two days. When the acne present is gone, the frequency of application is reduced to once a week. While specific embodiments of the invention have been described, it will be apparent to those skilled in the art that various changes and modifications can be made to the invention without departing from the spirit and scope of the invention. It is believed that all such modifications that fall within the scope of the invention are covered by the appended claims.

────────────────────────────────────────────────── ─── Continuation of front page    (81) Designated countries EP (AT, BE, CH, DE, DK, ES, FR, GB, GR, IE, IT, LU, M C, NL, PT, SE), OA (BF, BJ, CF, CG , CI, CM, GA, GN, ML, MR, NE, SN, TD, TG), AP (KE, MW, SD, SZ, UG), AM, AU, BB, BG, BR, BY, CA, CN, C Z, EE, FI, GE, HU, JP, KG, KP, KR , KZ, LK, LR, LT, LV, MD, MG, MN, MX, NO, NZ, PL, RO, RU, SI, SK, T J, TT, UA, UZ, VN

Claims (1)

[Claims]   1. a) a safe and effective amount of a dipolar surfactant having the following structure: (R in the above formula¹Is an unsubstituted, saturated or unsaturated, straight-chain or Is a branched-chain alkyl; m is an integer from 1 to 3; n is 0 or 1;² And R^ThreeIs independently 1 to 3 carbons, unsubstituted or monosubstituted with hydroxy. Saturated linear alkyl having an elementary atom; R^FourHas 1 to 5 carbon atoms, non- Saturated or unsaturated, linear or branched chain substituted or hydroxy-monosubstituted Rukilen; X is CO₂, SO_ThreeAnd SO_FourSelected from the group consisting of),   b) a safe and effective amount of benzoyl peroxide, and   c) Local carrier An anti-acne composition useful for topical application, characterized in that it comprises:   2. (A) the concentration of benzoyl peroxide is 0.1 to 10%,   (B) The concentration of the dipolar surfactant is 0.1 to 10%, The composition according to claim 1.   3. (A) R²And R^ThreeIs CH_Three, CH₂CH₂OH, CH₂CH₂CH₂OH And   (B) X is CO₂Or SO_ThreeAnd   (C) m is 2 or 3, The composition according to claim 1 or 2.   4. R^FourIs a saturated straight chain and X is CO₂Then 1 to 3 carbon atoms and X is SO_Three The composition of claim 3 having 2 to 4 carbon atoms.   5. a) R¹Is saturated linear alkyl having 11 to 18 carbon atoms,   b) R²And R^ThreeIs CH_ThreeAnd   c) R^FourX is CO₂Has one carbon atom, and R^FourX is SO_ThreeWhen three Has carbon atoms of   d) m is 3, and   e) n is 1, The composition according to claim 4.   6. (A) the concentration of benzoyl peroxide is 1 to 6%,   (B) The concentration of the dipolar surfactant is 1 to 6%, The composition according to any one of claims 1 to 5.   7. 7. Any one of claims 1-6, further comprising 1-6% glycolic acid. The composition according to Item.   8. Bipolar surfactants are behenyl betaine, cocoamidopropyl betaine, Cetylpropyl hydroxysultaine or cetyl betaine. A composition according to any one of the preceding claims.   9. (A) The amount of benzoyl peroxide is 0.004-0 when applied topically. . 1 mg / cm²Skin, and   (B) The amount of dipolar surfactant, when applied topically, is 0.004 to 0.1 m. g / cm²Is the skin, The composition according to any one of claims 1 to 8.   10. The ingredients are:   a) a safe and effective amount of a dipolar surfactant having the following structure: (R in the above formula¹Is an unsubstituted, saturated or unsaturated, straight-chain or Is a branched-chain alkyl; m is an integer from 1 to 3; n is 0 or 1;² And R^ThreeIs independently 1 to 3 carbons, unsubstituted or monosubstituted with hydroxy. Saturated linear alkyl having an elementary atom; R^FourHas 1 to 5 carbon atoms, non- Saturated or unsaturated, linear or branched chain substituted or hydroxy-monosubstituted Rukilen; X is CO₂, SO_ThreeAnd SO_FourSelected from the group consisting of),   b) a safe and effective amount of benzoyl peroxide, and   c) Local carrier A topical anti-acne composition according to claim 1 characterized in that Usage of various ingredients related to construction.