(WO2020202107) Isopropylcarbonate benzoyl peroxide compositions and methods of use 机翻标题: 暂无翻译,请尝试点击翻译按钮。

源语言标题
(WO2020202107) Isopropylcarbonate benzoyl peroxide compositions and methods of use
公开号/公开日
WO2020/202107 / 2020-10-08
申请号/申请日
WOIB2020/053223 / 2020-04-03
发明人
NADAU-FOURCADE KARINEBUGE JEAN-CHRISTOPHE;
申请人
NESTLE SKIN HEALTH;
主分类号
IPC分类号
A61K-008/38 A61K-031/216 A61P-017/10 A61Q-019/00 C07C-409/34
摘要
(WO2020/202107) Described herein are compositions comprising (i) Isopropylcarbonate Benzoyl Peroxide, (ii) an opacifier, and (iii) and a preserving agent that have good physical, chemical and microbiological stability and corresponding methods of use.
机翻摘要
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地址
代理人
代理机构
;
优先权号
2019US-62829507
主权利要求
(WO2020/202107) WHAT IS CLAIMED IS: 1. A topically applicable composition comprising:   i) Isopropylcarbonate Benzoyl Peroxide;   ii) an opacifier; and   iii) a preserving agent. 2. The topically applicable composition of claim 1 , wherein the composition comprises about 0.0001% to about 20%, about 0.001% to about 20%, about 0.01% to about 20%, about 0.1% to about 20%, about 0.1% to about 10%, about 0.1% to about 5%, about 2.5% to about 5% by weight of Isopropylcarbonate Benzoyl Peroxide. 3. The topically applicable composition of claim 1 or claim 2, wherein the composition comprises about 3% by weight of Isopropylcarbonate Benzoyl Peroxide. 4. The topically applicable composition of any one of claims 1-3, wherein the opacifier is bismuth oxychloride, titanium dioxide, fluorphlogopite, mica, iron oxide, nylon polymer, polymethyl methacrylate, boron nitride, kaolin, glycol distearate, styrene copolymer, a fatty alcohol, or any combination thereof. 5. The topically applicable composition of any one of claims 1-4, wherein the opacifier is titanium dioxide. 6. The topically applicable composition of claim 5, wherein the titanium dioxide is pharmaceutical grade or cosmetic grade. 7. The topically applicable composition of any one of claims 1-6, wherein the composition comprises about 0.1% to about 2.5% by weight of the opacifier. 8. The topically applicable composition of any one of claims 1-7, wherein the composition comprises about 0.4% by weight of the opacifier. 9. The topically applicable composition of any one of claims 1-8, wherein the preserving agent is phenoxyethanol, potassium sorbate, benzyl alcohol, methyl paraben, chlorhexidinedigluconate, chloroxylenol, chlorphenesin, dehydroacetic acid, diazolidinyl urea, DMDM hydantoin, ethylparaben, iodopropynyl butylcarbamate, methylisothiazobnone, propyllparaben, phenoxyethanol, phenoxyisopropanol, polyaminopropyl biguianide, sodium benzoate, salicylic acid, or any combination thereof. 10. The topically applicable composition of any one of claims 1-9, wherein the preserving agent is phenoxyethanol. 11. The topically applicable composition of any one of claims 1-10, wherein the composition comprises about 0.1% to about 0.8% by weight of the preserving agent. 12. The topically applicable composition of any one of claims 1-11, wherein the composition comprises about 0.4% or about 0.8% by weight of the preserving agent. 13. The topically applicable composition of any one of claims 1-12, wherein the composition further comprises a surfactant. 14. The topically applicable composition of claim 13, wherein the surfactant is docusate sodium (diethylhexyl sodium sulfosuccinate), poloxamer, PEG ether, PPG ester, alkyl polyglucoside, sorbitan ester, ethoxylated sorbitan ester, alcohol sulfate, ethoxylated alcohol sulfate, alkyl benzene sulfonate, alpha olefin sulfonate, sulfosuccinate, isethionate ester, taurate, alkyl betaine, alkyl amidopropyl betaine, amphoacetate, or alkyl sultaine. 15. The topically applicable composition of claim 13 or claim 14, wherein the composition comprises about 0.05% by weight of the surfactant. 16. The topically applicable composition of any one of claims 1-15, wherein the composition further comprises a humectant. 17. The topically applicable composition of claim 16, wherein the humectant is glycerol. 18. The topically applicable composition of claim 16 or claim 17, wherein the composition comprises about 4% by weight of the humectant.19. The topically applicable composition of any one of claims 1-18, wherein the composition further comprises a liquid wetting surfactant. 20. The topically applicable composition of claim 19, wherein the liquid wetting surfactant is a poloxamer. 21. The topically applicable composition of claim 20, wherein the liquid wetting surfactant is poloxamer 124. 22. The topically applicable composition of any one of claims 19-21, wherein the composition comprises about 0.2% by weight of the liquid wetting surfactant. 23. The topically applicable composition of any one of claims 1-22, wherein the composition further comprises a gelling agent. 24. The topically applicable composition of claim 23, wherein the gelling agent comprises acrylamide, sodium acryloyldimethyl taurate copolymer, isohexadecane and polysorbate 80 (SIMULGEL™ 600). 25. The topically applicable composition of claim 23, wherein the gelling agent comprises hydroxy ethyl acrylate, sodium acryloyldimethyl taurate copolymer, isohexadecane and polysorbate 60 (SIMULGEL™ INS 100). 26. The topically applicable composition of claim 23, wherein the gelling agent comprises hydroxy ethyl acrylate and sodium acryloyldimethyl taurate copolymer (SEPINOV™ EMTIO). 27. The topically applicable composition of any one of claims 24-26, wherein the gelling agent is pharmaceutical grade or cosmetic grade. 28. The topically applicable composition of any one of claims 23-27, wherein the composition comprises about 0.1% to about 10% by weight of the gelling agent. 29. The topically applicable composition of any one of claims 23-28, wherein the composition comprises about 4% by weight of the gelling agent.30. The topically applicable composition of any one of claims 1-29, wherein the composition further comprises a pro-penetrating agent. 31. The topically applicable composition of claim 30, wherein the pro-penetrating agent is propylene glycol, dipropylene glycol, propylene glycol dipelargonate, lauroglycol, an alcohol, an alkylmethyl sulfoxide, a polyol, oleic acid, isopropyl myristate, decylmethyl sulfoxide, DMSO, urea, or ethoxydiglycol. 32. The topically applicable composition of claim 30, wherein the pro-penetrating agent is propylene glycol. 33. The topically applicable composition of any one of claims 30-32, wherein the composition comprises about 4% by weight of the pro-penetrating agent. 34. The topically applicable composition of any one of claims 1-33, wherein the composition further comprises a sequestering agent. 35. The topically applicable composition of claim 34, wherein the sequestering agent is disodium ethylenediaminetetraacetic acid (EDTA), dihydroxyethylglycine, citric acid, tartaric acid or a derivative or salt thereof. 36. The topically applicable composition of claim 34 or claim 35, wherein the sequestering agent is disodium ethylenediaminetetraacetic acid (EDTA). 37. The topically applicable composition of any one of claims 34-36, wherein the composition comprises about 0.1% to about 0.5% by weight of the sequestering agent. 38. The topically applicable composition of any one of claims 34-37, wherein the composition comprises about 0.1% or about 0.2% by weight of the sequestering agent. 39. The topically applicable composition of any one of claims 1-38, wherein the composition further comprises a vehicle. 40. The topically applicable composition of claim 39, wherein the vehicle is purified water.41. The topically applicable composition of any one of claims 1-40, wherein the composition is further formulated as a gel. 42. The topically applicable composition of any one of claims 1-40, wherein the composition is further formulated as a cream. 43. The topically applicable composition of any one of claims 1-43, wherein the composition further comprises a keratolytic agent, an oil, an antioxidant, a skin conditioning agent, or any combination thereof. 44. The topically applicable composition of claim 43, wherein the keratolytic agent is lactic acid, glycolic acid, malic acid, phytic acid, silver or a silver solution. 45. The topically applicable composition of claim 43, wherein the oil comprises mineral oil, hydrogenated polyisobutene, squalene, polydecene, or any combination thereof. 46. The topically applicable composition of claim 43, wherein the antioxidant comprises butylated hydroxytoluene, DL alpha tocopherol, ascorbyl palmitate, or any combination thereof. 47. The topically applicable composition of claim 43, wherein the skin conditioning agent comprises silica beads, methyl methacrylate cross polymer, nylon polymer, mica, polymethyl methacrylate, titanium dioxide, or any combination thereof. 48. A topically applicable composition comprising:   i) Isopropylcarbonate Benzoyl Peroxide;   ii) titanium dioxide as an opacifier;   iii) phenoxy ethanol as a preserving agent;   iv) docusate sodium (diethylhexyl sodium sulfosuccinate) as a surfactant;   v) glycerol as a humectant;   vi) poloxamer 124 as a liquid wetting surfactant;   vii) acrylamide/sodium acryloyldimethyl taurate copolymer and isohexadecane and polysorbate 80 as a gelling agent;   viii) propylene glycol as a pro-penetrating agent;ix) disodium EDTA as a sequestering agent; and   x) purified water as a vehicle. 49. A topically applicable composition comprising:   i) about 3% by weight of Isopropylcarbonate Benzoyl Peroxide;   ii) about 0.4% by weight of titanium dioxide as an opacifier;   iii) about 0.4% by weight of phenoxy ethanol as a preserving agent;   iv) about 0.05% by weight of docusate sodium (diethylhexyl sodium sulfosuccinate) as a surfactant;   v) about 4% by weight of glycerol as a humectant;   vi) about 0.2% by weight of poloxamer 124 as a liquid wetting surfactant;   vii) about 4% by weight of acrylamide/sodium acryloyldimethyl taurate copolymer and isohexadecane and polysorbate 80 as a gelling agent   viii) about 4% by weight of propylene glycol as a pro-penetrating agent;   ix) about 0.1% or about 0.2% by weight of disodium EDTA as a sequestering agent; and x) purified water as a vehicle. 50. The topically applicable composition of any one of claims 1-49, wherein the minimum amount of Isopropylcarbonate Benzoyl Peroxide remaining at the end of the shelf life of the composition is from about 0.001% to about 5%, about 0.001% to about 2%, about 0.001% to about 1.4%, about 0.5% to about 2%, or about 0.5% to about 1.4% by weight. 51. The topically applicable composition of claim 50, wherein the minimum amount of Isopropylcarbonate Benzoyl Peroxide remaining at the end of the shelf life of the composition is from about 1.4% by weight. 52. A method for producing an Isopropylcarbonate Benzoyl Peroxide aqueous gel, which method comprises the steps of:   i) solubilizing a sequestering agent in aqueous solution to produce the main phase;ii) preparing a disaggregation medium comprising Isopropylcarbonate Benzoyl Peroxide by dispersing Isopropylcarbonate Benzoyl Peroxide, propylene glycol, glycerol and liquid wetting surfactant in water to produce medium A; and   iii) adding titanium dioxide to the main phase;   iv) adding a first portion of gelling agent to the main phase;   v) adding medium A to the main phase;   vi) adding of phenoxyethanol to the main phase;   vii) solubilizing docusate sodium in water to provide solubilized docusate sodium   followed by addition of the solubilized docusate sodium to the main phase by gentle agitation; and   viii) adding a second portion of gelling agent to the main phase,   whereby a gel is formed. 53. The method of claim 52, wherein the Isopropylcarbonate Benzoyl Peroxide from step ii) is subjected to a colloid mill. 54. A method for treating common acne, comedones, polymorphous acne, nodulocystic acne, acne conglobata, or secondary acne afflicting the skin of an individual in need of such treatment, comprising topically administering to the individual a topically applicable composition according to any one of claims 1-51. 55. A regime or regimen for reducing the number of acne lesions, comprising administering to an individual afflicted therewith an effective amount of a composition according to any one of claims 1-51. 56. The regime or regimen according to claim 55, the acne lesions being of inflammatory and/or non-inflammatory type. 57. A regime or regimen for controlling breakouts, comprising administering to an individual afflicted therewith an effective amount of a composition according to any one of claims 1-51.58. The regime or regimen according to claim 57, wherein controlling breakouts includes purifying and cleansing the skin, un-clogging pores, reducing oil, hydrating skin, and a combination thereof. 59. A regimen for treatment of acne vulgaris, comprising, i) cleaning skin;   ii) applying a topically applicable composition according to any of claims 1-51 to the skin; and   iii) applying a moisturizing treatment to the skin. 60. A regimen for treatment of acne vulgaris, comprising,   i) cleaning skin; and   ii) applying a topically applicable composition according to any of claims 1-51 to the skin. 61. The regimen for treatment of acne vulgaris as defined by claim 59 or claim 60, comprising administering said topically applicable composition for at least twelve (12) months. 62. The regimen for the treatment of acne vulgaris as defined by claim 59 or claim 60, comprising administering said topically applicable composition for at least nine (9) months. 63. The regimen for the treatment of acne vulgaris according to any one of claims 59-62, comprising administering said topically applicable composition once or twice a day. 64. The regimen for the treatment of acne vulgaris according to any one of claims 59-62, comprising administering said topically applicable composition every two (2) days. 65. The regimen for the treatment of acne vulgaris according to any one of claims 59-64, comprising administering said topically applicable composition in the evening after washing said affected skin area.66. The regimen for the treatment of acne vulgaris according to any one of claims 59-64, said affected skin area containing from 20 to 100 non- inflammatory lesions, 20 to 50 inflammatory lesions, and no active nodules or cysts. 67. A kit comprising   a) a topically applicable composition according to any one of claims 1-51; and b) a topical cleanser and/or a topical moisturizer. 68. The kit according to claim 67, where the facial cleaner and/or the facial moisturizer comprise salicylic acid. 69. The kit according to claim 68, wherein the salicylic acid is present in an amount from 0.1 -2.5%. 70. The kit according to claim 68, wherein the salicylic acid is present in an amount of 0.5%. 71. The kit according to claim 68, wherein the salicylic acid is present in an amount of 2%. 72. The kit according to claim 67, where the facial cleaner and/or the facial moisturizer comprise benzoyl peroxide. 73. The kit according to claim 72, wherein the benzoyl peroxide is present in an amount from 0.1 -2.5%. 74. The kit according to claim 72, wherein the benzoyl peroxide is present in an amount of 0.5%. 75. The kit according to claim 72, wherein the benzoyl peroxide is present in an amount of 2%. 76. The kit according to claim 67, where the facial cleaner and/or the facial moisturizer comprise adapalene. 77. The kit according to claim 76, wherein the adapalene is present in an amount from 0.1-  1824 3218 7320.178. The kit according to claim 76, wherein the adapalene is present in an amount of 1%.
法律状态
PENDING
专利类型码
A1
国别省市代码
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