Details for Patent: 6,319,913
✉ Email this page to a colleague
Title: | Penetration enhancing and irritation reducing systems |
Abstract: | 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. |
Inventor(s): | Mak; Vivien H. W. (Menlo Park, CA), Grayson; Stephen (San Rafael, CA) |
Assignee: | Cellegy Pharmaceuticals, Inc. (South San Francisco, CA) |
Filing Date: | Nov 09, 1998 |
Application Number: | 09/189,090 |
Claims: | 1. A method for administering a topically or systemically active agent with increased penetration, said method comprising: topically administering to a mammal a composition comprising: a) an active agent having a concentration of about 0.1% to about 2%, wherein said active agent is a member selected from the group consisting of testosterone, estradiol, derivatives thereof and the mixture thereof; b) a penetration-enhancing system consisting essentially of (i) a membrane fluidizer comprising oleic acid; (ii) a C.sub.1 -C.sub.4 alcohol; and (iii) a glycol said composition having a pH value of between about 4 to about 8, thereby administering a topically or systemically active agent with increased penetration. 2. A method in accordance with claim 1, wherein said penetration-enhancing system further comprises (iv) a gelling agent. 3. A method in accordance with claim 1, wherein said active agent is testosterone. 4. A method in accordance with claim 1, wherein said active agent is testosterone propionate. 5. A method for reducing inflammation associated with topical application of a topically or systemically active agent, said method comprising: topically administering to a mammal a composition comprising: a) an active agent having a concentration of about 0.1% to about 2%, wherein said active agent is a member selected from the group consisting of testosterone, estradiol, derivatives thereof and the mixture thereof; b) a penetration-enhancing system consisting essentially: (i) a membrane fluidizer comprising oleic acid; (ii) a C.sub.1 -C.sub.4 alcohol; and (iii) a glycol said composition having a pH value of between about 4 to about 8, thereby reducing inflammation associated with a topical application of a topically or systemically active agent. 6. A method in accordance with claim 5, wherein said penetration-enhancing system further comprises (iv) a gelling agent. 7. A method in accordance with claim 6, wherein said active agent is a member selected from the group consisting of testosterone, testosterone propionate and mixtures thereof. 8. A method in accordance with claim 7, wherein said active agent is testosterone propionate. 9. A method in accordance with claim 1, wherein said pH value is between about 4.5 to about 6.5. 10. A method in accordance with claim 1, wherein said active agent is present in a concentration selected from the group consisting of 0.5%, 1.00%, 1.25%, 1.50% and 2.00% weight to weight of said composition. 11. A method in accordance with claim 1, wherein said C.sub.1 -C.sub.4 alcohol is isopropanol. 12. A method in accordance with claim 1, wherein said glycol is propylene glycol. 13. A method in accordance with claim 1, wherein said gelling agent is Carbopol 1342. 14. A method in accordance with claim 1, wherein said penetration enhancing system fmal urther comprises an irritation reducing agent. 15. A method in accordance with claim 1, wherein said active agent is a mixture of testosterone and estradiol. 16. A method in accordance with claim 5, wherein said active agent is testosterone. 17. A method in accordance with claim 5, wherein said active agent is a mixture of testosterone and estradiol. 18. A method in accordance with claim 5, wherein said penetration enhancing system further comprises an iritation reducing agent. 19. A method for administering a topically or systemically active agent with increased penetration, said method comprising: topically administering to a mammal a composition comprising: a) testosterone or a derivative thereof having a concentration of about 0.1% to about 2%; b) a penetration-enhancing system comprising: (i) oleic acid; (ii) a C.sub.3 alcohol; and (iii) propylene glycol thereby administering a topically or systemically active agent with increased penetration. 20. A method in accordance with claim 19, wherein testosterone or a derivative thereof is present in a concentration selected from the group consisting of 0.5%, 1.00%, 1.25%, 1.50% and 2.00% weight to weight of said composition. 21. A method in accordance with claim 19, wherein said penetration-enhancing system further comprises (iv) a gelling agent. 22. A method for administering a topically or systemically active agent with increased penetration, said method comprising: topically administering to a mammal a composition comprising: a) estradiol or a derivative thereof having a concentration of about 0.1% to about 10%; b) a penetration-enhancing system comprising: (i) oleic acid; (ii) a C.sub.3 alcohol; and (iii) propylene glycol, thereby administering a topically or systemically active agent with increased penetration. 23. A method in accordance with claim 22, wherein estradiol or a derivative thereof is present from about 0.1% to about 5% weight to weight of said composition. 24. A method in accordance with claim 22, wherein estradiol or a derivative thereof is present from about 1% to about 2% weight to weight of said composition. 25. A method in accordance with claim 22, wherein estradiol or a derivative thereof is present in a concentration selected from the group consisting of 0.5%, 1.00%, 1.25%, 1.50% and 2.00% weight to weight of said composition. 26. A method in accordance with claim 22, wherein said penetration-enhancing system further comprises (iv) a gelling agent. |