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Kafe 바로가기국가/구분 | United States(US) Patent 등록 |
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국제특허분류(IPC7판) |
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출원번호 | US-0745417 (2008-12-01) |
등록번호 | US-9439857 (2016-09-13) |
국제출원번호 | PCT/IB2008/003908 (2008-12-01) |
§371/§102 date | 20101109 (20101109) |
국제공개번호 | WO2009/069006 (2009-06-04) |
발명자 / 주소 |
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출원인 / 주소 |
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대리인 / 주소 |
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인용정보 | 피인용 횟수 : 11 인용 특허 : 557 |
The present invention relates to foamable compositions for treating acne comprising benzoyl peroxide; to a therapeutic kit comprising such compositions; and to a method of treating acne using such compositions.
1. A foamable composition in an aerosol packaging assembly for treating skin comprising a prefoam emulsion composition and a liquefied or compressed gas propellant, the prefoam emulsion composition comprising: a) i) a suspended or entrapped active agent selected from the group consisting of benzoyl
1. A foamable composition in an aerosol packaging assembly for treating skin comprising a prefoam emulsion composition and a liquefied or compressed gas propellant, the prefoam emulsion composition comprising: a) i) a suspended or entrapped active agent selected from the group consisting of benzoyl peroxide, imiquimod, acyclovir, zinc oxide, titanium oxide, an antibiotic, and a corticosteroid; orii) an encapsulated or entrapped or suspended drug insoluble in the prefoam emulsion; andb) a carrier comprising: i) one or more surface-active agents;ii) about 0.01% to about 1% by weight of the emulsion composition of at least one pH sensitive polymeric additive comprising a polyacrylic acid polymer;iii) a hydrophobic solvent, wherein the hydrophobic solvent comprises at least 1% by weight of the emulsion composition of an oil;iv) water; andv) a buffer system, wherein up to about 2% by weight of the emulsion composition comprises the buffer system,wherein the buffer system is at a pH less than the pH of the prefoam emulsion before addition of the buffer system and is selected to provide a prefoam composition that is fluid at room temperature and that has a viscosity of less than about 8000 centipoises; wherein the liquefied or compressed gas propellant is at a concentration of about 3% to about 25% by weight of the foamable composition,wherein the pH sensitive polymeric additive is reversibly susceptible to buffer or pH adjuster, and the polymer together with the buffer system contributes to holding the active agent homogeneously dispersed in the foamable composition over a prolonged time,wherein the foamable composition is fluid at room temperature; andwherein the composition forms a breakable foam upon dispensing in which the active agent is homogenously dispersed. 2. The composition of claim 1, wherein the foam produced from the foamable composition has an average bubble size of less than about 150 microns; and/or wherein the foam produced has a density range between about 0.02 g/mL and about 0.1 g/mL. 3. The composition of claim 1, wherein the prefoam emulsion composition further comprises a pH adjusting component selected from the group consisting of a base and a buffer system, said pH adjusting component selected to be able to gel the polymeric additive. 4. The composition of claim 3, wherein the pH of the prefoam emulsion composition is between about 4.0 and about 6.0. 5. The composition of claim 4, wherein the buffer system is at a pH less than the pH of the prefoam emulsion before addition of the buffer and is selected to provide a liquid prefoam emulsion. 6. The composition of claim 1, wherein the buffer system is selected from the group consisting of citric acid, sodium citrate, lactic acid, ammonium lactate, and mixtures of any two or more thereof. 7. The composition of claim 1, wherein the prefoam emulsion composition further comprises about 5% to about 30% by weight of a moisturizing complex comprising a moisturizing compound and a salt of 2-pyrrolidone-5-carboxylic acid (PCA),wherein the hydrophobic solvent comprises mineral oil and a silicone oil,wherein the prefoam emulsion composition improves the hydration of skin after 7 hours by at least about 20%. 8. The composition of claim 7, wherein the hydrophobic solvent is at a concentration from about 1% to about 15% by weight of the prefoam emulsion. 9. The foamable composition of claim 7, wherein the suspended or entrapped active agent/drug is benzoyl peroxide; wherein the buffer system is selected to provide a prefoam composition that is fluid at room temperature, said prefoam composition having a viscosity of less than about 8000 centipoises; andwherein the moisturizing complex enhances the stability of the foamable composition and/or reduces skin dryness or irritation associated with use of benzoyl peroxide. 10. The composition of claim 7, where the moisturizing complex comprises glycerin and a salt of PCA. 11. The composition of claim 7, wherein the prefoam emulsion composition comprises about 5% to about 15% by weight of the moisturizing complex. 12. The composition of claim 1, wherein the composition further comprises a phase-change polymer. 13. The composition of claim 1, wherein the one or more surface-active agents comprises between about 0.1% and about 5% by weight non ionic surface-active agents selected from the group consisting of steareth-21, steareth-2, steareth 20, polysorbate 80, polysorbate 60, polysorbate 20, ceteth 20, PEG 40-stearate, PEG 100-stearate, PEG-30 dipolyhydroxystearate, sorbitan stearate, sorbitan palmitate, sorbitan laurate, sorbitan monooleate, glyceryl stearate, laureth 4, ceteareth 20, macrogol cetostearyl ether, ceteth 2, sucrose distearate, polyoxyethylene (100) stearate, and mixtures of any two or more thereof. 14. The composition of claim 1, wherein the polymeric additive further comprises a polymeric agent selected from the group consisting of methylcellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxyethyl cellulose, methylhydroxyethylcellulose, hydroxyethylcarboxymethylcellulose, carboxymethylcellulose, sodium carboxymethylcellulose, xanthan gum, guar gum, carrageenan gum, locust bean gum, tragacanth gum and mixtures of any two or more thereof. 15. The composition of claim 1, wherein the prefoam emulsion composition further comprises about 0.1% to about 5% by weight of a therapeutically active foam adjuvant selected from the group consisting of fatty alcohols having 15 or more carbons in their carbon chain; fatty acids having 16 or more carbons in their carbon chain; fatty alcohols derived from beeswax and including a mixture of alcohols, a majority of which has at least 20 carbon atoms in their carbon chain; fatty alcohols having at least one double bond; fatty acids having at least one double bond; branched fatty alcohols; branched fatty acids; fatty acids substituted with a hydroxyl group; cetyl alcohol; stearyl alcohol; arachidyl alcohol; behenyl alcohol; 1-triacontanol; hexadecanoic acid; stearic acid; arachidic acid; behenic acid; octacosanoic acid; 12-hydroxy stearic acid and mixtures of any two or more thereof. 16. The composition of claim 1, wherein the prefoam emulsion composition further comprises at least one additional therapeutic agent selected from the group consisting of a steroidal anti-inflammatory agent, an immunosuppressive agent, an immunomodulator, an immunoregulating agent, a hormonal agent, an androgen, an estrogen, a prostaglandin, an antiandrogen agent, a testosterone inhibitor, a dihydrotestosterone inhibitor, an anti biotic agent, an antifungal agent, an antiviral agent, an antiparasitic agent, a retinoid, vitamin A, a vitamin A derivative, vitamin B, a vitamin B derivative, vitamin C, a vitamin C derivative, vitamin D, a vitamin D derivative, vitamin E, a vitamin E derivative, vitamin F, a vitamin F derivative, vitamin K, a vitamin K derivative, a wound healing agent, a disinfectant, an anesthetic, an antiallergic agent, a keratolytic agent, urea, a urea derivative, an alpha hydroxyl acid, lactic acid, glycolic acid, a beta-hydroxy acid, a protein, a peptide, a neuropeptide, an allergen, an immunogenic substance, a haptene, an oxidizing agent, an antioxidant, a dicarboxylic acid, azelaic acid, sebacic acid, adipic acid, fumaric acid, a retinoid, an antiproliferative agent, an anticancer agent, a photodynamic therapy agent, benzoyl chloride, calcium hypochlorite, magnesium hypochlorite, an anti-wrinkle agent, a radical scavenger, a metal, silver, a metal oxide, titanium dioxide, zinc oxide, zirconium oxide, iron oxide, silicone oxide, an organo-metallic compound, an organo-boron compound, an organo-berrilium compound, talc, carbon, an anti wrinkle agent, a skin whitening agent, a skin protective agent, a masking agent, an anti-wart agent, a refatting agent, a lubricating agent and mixtures of any two or more thereof; and wherein optionally the composition includes a stabilizing agent which acts as an effective barrier to a possible degradative interaction of the benzoyl peroxide and the at least one additional therapeutic agent. 17. The composition of claim 1, wherein the encapsulation or entrapping agent or particle is selected from the group comprising microsponges, polymer microspheres, zinc oxide, titanium oxide, silicone oxide and mixtures of any two or more thereof. 18. The composition of claim 1, further comprising a moisturizing complex, wherein the amount of hydrophobic solvent is about 1% to about 15% by weight of the prefoam emulsion composition. 19. The composition of claim 1, wherein the hydrophobic solvent is selected from the group consisting of a mineral oil, aliphatic, naphthalenic, and aromatic liquid hydrocarbons that derive from petroleum, a liquid oil originating from vegetable, marine or animal source, a saturated, unsaturated or polyunsaturated oil, a corn oil, a soybean oil, a canola oil, a cottonseed oil, a coconut oil, a sesame oil, a sunflower oil, a borage seed oil, a syzigium aromaticum oil, a hempseed oil, a herring oil, a cod-liver oil, a salmon oil, a flaxseed oil, a wheat germ oil, an evening primrose oil, a polyunsaturated oil containing poly-unsaturated fatty acids, omega-3 fatty acids, omega-6 fatty acids, linoleic acid, linolenic acid, gamma-linoleic acid (GLA), eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), an omega-3 oil, an omega-6 oil, a liquid hydrophobic plant-derived oil, a silicone oil, a non-volatile silicone, a polyalkyl siloxane, a polyaryl siloxane, a polyalkylaryl siloxane, a polyether siloxane copolymer, a polydimethylsiloxane, a dimethicone, a poly(dimethylsiloxane)-(diphenyl-siloxane) copolymer, a cyclic or linear polydimethylsiloxane containing from about 3 to about 9, or from about 4 to about 5, silicon atoms, a volatile silicone, acyclomethicone, and mixtures of any two or more thereof. 20. The composition of claim 1, wherein the prefoam emulsion composition comprises about 0.2% to about 0.85% by weight of the at least one pH sensitive polymeric additive. 21. The composition of claim 1, wherein the oil comprises a silicone oil. 22. The composition of claim 21, wherein the silicone oil is selected from a group consisting of a dimethicone, a cyclomethicone, a polyalkyl siloxane, a polyaryl siloxane, a polyalkylaryl siloxane, a polyether siloxane copolymer, a poly(dimethylsiloxane)-(diphenyl-siloxane) copolymer, and mixtures of any two or more thereof. 23. The composition of claim 1, wherein the amount of oil is about 1% to about 15% by weight of the emulsion composition. 24. The composition of claim 23, wherein the oil is selected from the group consisting of a mineral oil, a silicone oil, a jojoba oil, a MCT oil and mixtures of two or more thereof. 25. The composition of claim 24, wherein the surface-active agent comprises a combination of at least one non-ionic surfactant having HLB of less than 9 and at least one non-ionic surfactant having HLB of equal or more than 9. 26. The composition of claim 25, wherein the surface-active agent comprises at least two or more of a monoglyceride, a polyoxyethylene fatty acid ester, and a polysorbate. 27. The composition of claim 26, wherein the non-ionic surfactant having HLB of less than 9 and at least one non-ionic surfactant having HLB of equal or more than 9 are at a ratio of between 1:8 and 8:1, or at a ratio of 4:1 to 1:4. 28. The composition of claim 26, wherein the weighted average HLB of the combination of non-ionic surfactants is between about 5 and about 18. 29. The composition of claim 26, wherein the surface-active agent comprises two or more of glyceryl stearate, polysorbate 60 and PEG 40 stearate. 30. The composition of claim 1, wherein the prolonged time is at least two months. 31. The composition of claim 1, wherein the prolonged time is at least three months. 32. The composition of claim 1, wherein the prolonged time is at least six months. 33. A foamable composition in an aerosol packaging assembly comprising a prefoam emulsion composition and a liquefied or compressed gas propellant, the prefoam emulsion composition comprising: i. a suspended solid active agent;ii. one or more surface-active agents;iii. about 0.01% to about 1% by weight of the emulsion composition of at least one pH sensitive polymeric additive comprising a polyacrylic acid polymer;iv. about 5% to about 15% by weight of the emulsion composition of a moisturizing complex;v. a hydrophobic solvent;vi. water; andvii. a buffer system, wherein up to about 2% by weight of the emulsion composition comprises the buffer system,wherein the buffer system is at a pH less than the pH of the prefoam emulsion before addition of the buffer system and is selected to provide a prefoam composition that is fluid at room temperature, said prefoam composition having a viscosity of less than about 8000 centipoises (cps);wherein the pH sensitive polymeric additive is reversibly susceptible to buffer or pH adjuster, and the polymer together with the buffer system contributes to holding the active agent homogeneously dispersed in the foamable composition over a prolonged time,wherein the liquefied or compressed gas propellant is at a concentration of about 3% to about 25% by weight of the foamable composition;wherein the foamable composition is fluid at room temperature;wherein the suspended solid active agent has an average particle size of less than about 35 microns;wherein the composition further comprises at least one organic carrier selected from the group consisting of an organic polar solvent, an emollient and mixtures thereof, at a concentration of about 2% to about 50% by weight;wherein the at least one organic carrier comprises a penetration enhancer selected from the group consisting of propylene glycol, butylene glycols, hexylene glycol, glycerol, pentaerythritol, sorbitol, mannitol, oligosaccharides, dimethyl isosorbide, monooleate of ethoxylated glycerides having about 8 to 10 ethylene oxide units, polyethylene glycol 200-600, transcutol, glycofurol and cyclodextrins; andwherein the composition forms a breakable foam upon dispensing in which the active agent is homogenously dispersed. 34. The foamable composition of claim 33, wherein the polar solvent is about 1% to about 25% by weight of the emulsion composition and the polar solvent is selected from the group consisting of polyols, glycerol, propylene glycol, hexylene glycol, diethylene glycol, propylene glycol n-alkanols, terpenes, di-terpenes, tri-terpenes, terpen-ols, limonene, terpene-ol, 1-menthol, dioxolane, ethylene glycol, sulfoxides, dimethylsulfoxide, dimethylformanide, methyl dodecyl sulfoxide, dimethylacetamide, monooleates of ethoxylated glycerides with 8 to 10 ethylene oxide units, azone (1-dodecylazacycloheptan-2-one), 2-(n-nonyl)-1,3-dioxolane, isopropyl myristate, isopropyl palmitate, ethyl acetate, butyl acetate, methyl proprionate, capric/caprylic triglycerides, octylmyristate, dodecyl-myristate, lauryl alcohol, lauric acid, lauryl lactate, ketones, amides, acetamide oleates, triolein, alkanoic acids, caprylic acid, lactam compounds, alkanols, dialkylamino acetates, a polyethylene glycol, PEG 200, PEG 300, PEG 400, PEG600, PEG 4000, PEG 6000, PEG 10000 and mixtures of any two or more thereof. 35. The composition of claim 33, wherein the prefoam emulsion composition further comprises a pH adjusting component selected from the group consisting of a base and a buffer system, said pH adjusting component selected to be able to gel the polymeric additive. 36. A method of making the foamable composition of claim 35 comprising: a) forming the prefoam emulsion comprising the active agent, the one or more surface-active agents; the at least one polymeric additive; the hydrophobic solvent; the pH adjusting component; the moisturizing complex; and the water, wherein the aqueous phase of the prefoam emulsion has a thickness sufficient to suspend the active agent;b) adding the buffer system to the prefoam emulsion to reduce the viscosity of the prefoam emulsion; andc) introducing the liquefied or compressed gas propellant to the prefoam emulsion to obtain a foamable composition having a stable suspended active solid and that is fluid at room temperature. 37. The method of claim 36, wherein the prefoam emulsion has a pH in the range from 4 to 6 or has a pH of less than about 5. 38. The method of claim 36, wherein the foamable composition forms a breakable foam upon dispensing in which the active agent is homogenously dispersed and wherein the foam produced from the foamable composition has an average bubble size of less than about 150 microns. 39. The method of claim 36, wherein the hydrophobic solvent is selected from the group consisting of a mineral oil, aliphatic, naphthalenic, and aromatic liquid hydrocarbons that derive from petroleum, a liquid oil originating from vegetable, marine or animal source, a saturated, unsaturated or polyunsaturated oil, a corn oil, a soybean oil, a canola oil, a cottonseed oil, a coconut oil, a sesame oil, a sunflower oil, a borage seed oil, a syzigium aromaticum oil, a hempseed oil, a herring oil, a cod-liver oil, a salmon oil, a flaxseed oil, a wheat germ oil, an evening primrose oil, a polyunsaturated oil containing poly-unsaturated fatty acids, omega-3 fatty acids, omega-6 fatty acids, linoleic acid, linolenic acid, gamma-linoleic acid (GLA), eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), an omega-3 oil, an omega-6 oil, a liquid hydrophobic plant-derived oil, a silicone oil, a non-volatile silicone, a polyalkyl siloxane, a polyaryl siloxane, a polyalkylaryl siloxane, a polyether siloxane copolymer, a polydimethylsiloxane, a dimethicone, a poly(dimethylsiloxane)-(diphenyl-siloxane) copolymer, a cyclic or linear polydimethylsiloxane containing from about 3 to about 9, or from about 4 to about 5, silicon atoms, a volatile silicone, acyclomethicone, and mixtures of any two or more thereof. 40. A method of treating a skin disorder, the method comprising administering a foam produced from a foamable composition of claim 1 topically onto the skin of a subject having said disorder.
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