Penetration enhancing and irritation reducing systems
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-009/70
A61K-008/02
A61K-031/56
출원번호
US-0389715
(2003-03-12)
발명자
/ 주소
Mak,Vivien H. W.
Grayson,Stephen
출원인 / 주소
Cellegy Pharmaceuticals Inc.
대리인 / 주소
Townsend and Townsend and Crew LLP
인용정보
피인용 횟수 :
1인용 특허 :
16
초록▼
This invention lies in the technology of transdermal and topical drug delivery. In particular, the present invention relates to enhancement of the penetration of transdermally or topically applied drugs and with the reduction of skin irritation that often accompanies transdermal and topical drug del
This invention lies in the technology of transdermal and topical drug delivery. In particular, the present invention relates to enhancement of the penetration of transdermally or topically applied drugs and with the reduction of skin irritation that often accompanies transdermal and topical drug delivery.
대표청구항▼
What is claimed is: 1. A composition for topical application having penetration-enhancing properties, said composition consisting essentially of: a) an active agent, wherein said active agent is estradiol or derivatives thereof having a concentration in about 0.1% to about 10%; b) a penetration-en
What is claimed is: 1. A composition for topical application having penetration-enhancing properties, said composition consisting essentially of: a) an active agent, wherein said active agent is estradiol or derivatives thereof having a concentration in about 0.1% to about 10%; b) a penetration-enhancing system consisting essentially of (i) a membrane fluidizer consisting essentially of oleic acid; (ii) a C1-C4 alcohol; and (iii) a penetration enhancing glycol; and c) a gelling agent, wherein said composition has a pH of about 4 to about 8. 2. The composition in accordance with claim 1, wherein said active agent is estradiol. 3. The composition in accordance with claim 1, wherein said active agent is present from about 0.1% to about 2% weight to weight of said composition. 4. The composition in accordance with claim 1, wherein said active agent is present from about 1% to about 2% weight to weight of said composition. 5. The composition in accordance with claim 1, wherein said oleic acid is present from about 0.1% to about 10% weight to weight of said composition. 6. The composition in accordance with claim 5, wherein said oleic acid is present from about 0.1% to about 5% weight to weight of said composition. 7. The composition in accordance with claim 1, wherein said C1-C4 alcohol is a member selected from the group consisting of ethanol, propanol, isopropanol and mixtures thereof. 8. The composition in accordance with claim 7, wherein said C1-C4 alcohol is ethanol. 9. The composition in accordance with claim 7, wherein said C1-C4 alcohol is propanol. 10. The composition in accordance with claim 7, wherein said C1-C4 alcohol is isopropanol. 11. The composition in accordance with claim 7, wherein said C1-C4 alcohol is a mixture of ethanol and isopropanol. 12. The composition in accordance with claim 1, wherein said C1-C4 alcohol is present from about 5% to about 65% weight to weight of said composition. 13. The composition in accordance with claim 12, wherein said C1-C4 alcohol is present from about 10% to about 40% weight to weight of said composition. 14. The composition in accordance with claim 12, wherein said C1-C4 alcohol is present from about 25% to about 35% weight to weight of said composition. 15. The composition in accordance with claim 1, wherein said glycol is a member selected from the group consisting of ethylene glycol, propylene glycol, butylene glycol and mixtures thereof. 16. The composition in accordance with claim 15, wherein said glycol is ethylene glycol. 17. The composition in accordance with claim 15, wherein said glycol is butylene glycol. 18. The composition in accordance with claim 15, wherein said glycol is propylene glycol. 19. The composition in accordance with claim 15, wherein said glycol is a mixture of ethylene glycol and butylene glycol. 20. The composition in accordance with claim 15, wherein said glycol is a mixture of propylene glycol and butylene glycol. 21. The composition in accordance with claim 1, wherein said glycol is present from about 25% to about 55% weight to weight of said composition. 22. The composition in accordance with claim 21, wherein said glycol is present from about 30% to about 40% weight to weight of said composition. 23. The composition in accordance with claim 1, wherein said gelling agent is a member selected from the group consisting of Carbopol 1342, Carbopol 940, Klucel and Klucel HF. 24. The composition in accordance with claim 23, wherein said gelling agent is Carbopol 1342. 25. The composition in accordance with claim 1, wherein said gelling agent is present from about 0.1% to about 10% weight to weight of said composition. 26. The composition in accordance with claim 25, wherein said gelling agent is present from about 0.1% to about 5% weight to weight of said composition. 27. The composition in accordance with claim 25, wherein said gelling agent is present from about 1% to about 3% weight to weight of said composition. 28. A transdermal patch, said transdermal patch consisting essentially of: a) estradiol or a derivative thereof having a concentration of about 0.1% to about 2%; and b) a penetration-enhancing system consisting essentially of: (i) oleic acid; (ii) a C3 alcohol; and (iii) propylene glycol. 29. A composition for topical application having penetration-enhancing properties, said composition consisting essentially of: a) an active agent, wherein said active agent is estradiol or derivatives thereof having a concentration of about 0.1% to about 2%; b) a penetration-enhancing system consisting essentially of (i) oleic acid; (ii) and C1-C4 alcohol; and (iii) a penetration enhancing glycol; c) a gelling agent; and d) an inert carrier, wherein said composition has a pH of about 4 to about 8. 30. The composition in accordance with claim 29, wherein said composition has a pH value between about 5 to about 6. 31. A method for treating a menopausal or postmenopausal symptom, said method comprising: topically administering to a mammal a composition according to claim 1, thereby treating said symptom. 32. The method in accordance with claim 31, wherein said composition has a pH value of between about 5 to about 6. 33. The method in accordance with claim 31, wherein said symptom is aging related changes to skin or mucous membranes. 34. The method in accordance with claim 31, wherein said symptom is skin pigmentation. 35. The method in accordance with claim 31, wherein said symptom is selected from skin roughness, wrinkles, furrows, fragility and atrophy. 36. The method in accordance with claim 31, wherein said symptom is nail thinning. 37. The method in accordance with claim 31, wherein said symptoms are hair thinning and/or fracturing.
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이 특허에 인용된 특허 (16)
Hale Ron L. (Woodside CA) Lu Amy (Los Altos CA) Solas Dennis (San Francisco CA) Selick Harold E. (Belmont CA) Oldenburg Kevin R. (Fremont CA) Zaffaroni Alejandro C. (Atherton CA), Compositions and methods for enhanced drug delivery.
Govil Sharad K. (Plantation FL) Sterner Dale (Pembroke Pines FL) Jones Stephen (Miami FL) Kennedy Geraldine (Plantation FL), Compositions for transdermal delivery of estradiol.
Patel Dinesh C. (Murray UT) Chang Yunik (Lakewood NJ), Penetration enhancement with binary system of oleic acid, oleins, and oleyl alcohol with lower alcohols.
Francoeur Michael L. (Los Altos CA) Potts Russell O. (San Francisco CA), Transdermal flux enhancing compositions to treat hypertension, diabetes and angina pectoris.
Quan Danyi (Salt Lake City UT) Deshpanday Ninad A. (Salt Lake City UT) Venkateshwaran Srinivasan (Salt Lake City UT) Ebert Charles D. (Salt Lake City UT), Triacetin as a penetration enhancer for transdermal delivery of a basic drug.
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