Penetration enhancing and irritation reducing systems
View Patent ↗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.
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 C 1 –C 4 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 C 1 –C 4 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 C 1 –C 4 alcohol is ethanol.
9. The composition in accordance with claim 7 , wherein said C 1 –C 4 alcohol is propanol.
10. The composition in accordance with claim 7 , wherein said C 1 –C 4 alcohol is isopropanol.
11. The composition in accordance with claim 7 , wherein said C 1 –C 4 alcohol is a mixture of ethanol and isopropanol.
12. The composition in accordance with claim 1 , wherein said C 1 –C 4 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 C 1 –C 4 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 C 1 –C 4 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 C 3 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 C 1 –C 4 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.