Claims
- 1. A topical composition comprising:
a topical anesthetic; a polymeric thickener selected from the group consisting of shear-thinning polysaccharide gums and shear-thinning polyacrylic acid polymers; a lipophilic component that is selected from the group consisting of an aliphatic C1 to C8 alcohol, an aliphatic C8 to C30 ester, a liquid polyol and a mixture thereof; water; and a buffer system that provides a buffered pH value for said composition in the range of about 3 to about 7.4.
- 2. The composition of claim 1 further comprising a vasoactive prostaglandin selected from the group consisting of PGE1, PGA1, PGB1, PGF1α, 19-hydroxy-PGA1, 19-hydroxy-PGB1, PGE2, PGA2, PGB2, 19-hydroxy-PGA2, 19-hydroxy-PGB2, PGE3, PGF3 and mixtures thereof.
- 3. The composition of claim 2 wherein the vasoactive prostaglandin is selected from the group consisting of prostaglandin E1, prostaglandin E2, a pharmaceutically acceptable salt thereof, a lower alkyl ester thereof and a mixture thereof.
- 4. The composition of claim 2 wherein the vasoactive prostaglandin is present in the amount of about 0.1 mg to about 0.5 mg.
- 5. The composition of claim 2 wherein the vasoactive prostaglandin is present in the amount of about 0.2 mg to about 0.3 mg.
- 6. The composition of claim 1 wherein the topical anesthetic is an aminoamide local anesthetic selected from the group consisting of lidocaine, bupivacaine, mepivacaine, dibucaine, propivacaine, etidocaine, tocainide, a pharmaceutically acceptable salt thereof and a mixture thereof.
- 7. The composition of claim 1 wherein the topical anesthetic is a local anesthetic selected from the group consisting of lidocaine, bupivacaine, dyclonine, a pharmaceutically acceptable salt thereof and a mixture thereof.
- 8. The composition of claim 1 wherein the topical anesthetic comprises about 0.01 to about 10 percent by weight based on the weight of the composition.
- 9. The composition of claim 1 wherein the polymeric thickener is a shear-thinning polyacrylic acid polymer.
- 10. The composition of claim 1 wherein the shear-thinning polysaccharide gum is a galactomannan gum.
- 11. The composition of claim 10, wherein the shear-thinning polysaccharide gum is a modified galactomannan gum.
- 12. The composition of claim 11 wherein the modified galactomannan gum is a modified guar gum.
- 13. The composition of claim 1 further comprising a penetration enhancer selected from the group consisting of an alkyl-(N-substituted amino) alkanoate, an alkyl-2-(N,N-disubstituted amino) alkanoate, an (N-substituted amino) alkanol alkanoate, an (N,N-disubstituted amino) alkanol alkanoate, a pharmaceutically acceptable salt thereof and a mixture thereof.
- 14. The composition of claim 13 wherein the penetration enhancer is dodecyl 2-(N,N-dimethylamino)-propionate or a pharmaceutically acceptable salt.
- 15. The composition of claim 1 wherein the lipophilic component comprises at least one glyceryl ester selected from the group consisting of monoglycerides, diglycerides, triglycerides, and mixtures thereof.
- 16. The composition of claim 1 wherein the lipophilic component comprises at least one glyceryl ester selected from the group consisting of glyceryl monooleate, triolein, trimyristin, tristearin, and mixtures thereof.
- 17. The composition of claim 1 wherein the composition further comprises an emulsifier selected from the group consisting of sucrose esters, polyoxyethylene sorbitan esters, long chain alcohols, and glyceryl esters.
- 18. The composition of claim 1 wherein the emulsifier comprises at least one glyceryl ester selected from the group consisting of glyceryl monooleate, triolein, trimyristin, tristearin, and mixtures thereof.
- 19. The composition of claim 1 wherein the composition further comprises up to about 5 percent myrtenol, based on the total weight of the composition.
- 20. The composition of claim 1 wherein the composition further comprises a preservative.
- 21. The method of claim 14 wherein the composition further comprises a fragrance.
- 22. A method of treating premature ejaculation in a patient needing such treatment comprising the steps of:
administering meatally an ejaculation latency prolonging amount of a semi-solid composition, comprising a topical anesthetic; a polymeric thickener selected from the group consisting of shear-thinning polysaccharide gums and shear-thinning polyacrylic acid polymers; a lipophilic component that is selected from the group consisting of an aliphatic C1 to C8 alcohol, an aliphatic C8 to C30 ester, a liquid polyol and a mixture thereof; water; and a buffer system that provides a buffered pH value for said composition in the range of about 3 to about 7.4.
- 23. The method of claim 22 wherein the composition further comprises a vasoactive prostaglandin selected from the group consisting of PGE1, PGA1, PGB1, PGF1α, 19-hydroxy-PGA1, 19-hydroxy-PGB1, PGE2, PGA2, PGB2, 19-hydroxy-PGA2, 19-hydroxy-PGB2, PGE3, PGF3 and mixtures thereof present in the amount of about 0.1 mg to about 0.5 mg.
- 24. The method of claim 22 wherein vasoactive prostaglandin is selected from the group consisting of prostaglandin E1, prostaglandin E2, a pharmaceutically acceptable salt thereof, a lower alkyl ester thereof and a mixture thereof.
- 25. The method of claim 22 wherein the vasoactive prostaglandin is present in the amount of about 0.2 mg to about 0.3 mg.
- 26. The method of claim 22 wherein the topical anesthetic is an aminoamide local anesthetic selected from the group consisting of lidocaine, bupivacaine, mepivacaine, dibucaine, propivacaine, etidocaine, tocainide, a pharmaceutically acceptable salt thereof and a mixture thereof.
- 27. The method of claim 22 wherein the topical anesthetic is a local anesthetic selected from the group consisting of lidocaine, bupivacaine, dyclonine, a pharmaceutically acceptable salt thereof and a mixture thereof.
- 28. The method of claim 22 wherein the topical anesthetic comprises about 0.01 to about 4 percent by weight based on the weight of the composition.
- 29. The method of claim 22 wherein the polymeric thickener is a shear-thinning polyacrylic acid polymer.
- 30. The method of claim 22 wherein the polymer is a shear-thinning polysaccharide gum.
- 31. The method of claim 22 wherein the shear-thinning polysaccharide gum is a galactomannan gum.
- 32. The method of claim 22, wherein the shear-thinning polysaccharide gum is a modified galactomannan gum.
- 33. The method of claim 32 wherein the modified galactomannan gum is a modified guar gum.
- 34. The method of claim 22 wherein the composition further comprises a penetration enhancer selected from the group consisting of an alkyl-(N-substituted amino) alkanoate, an alkyl-2-(N,N-disubstituted amino) alkanoate, an (N-substituted amino) alkanol alkanoate, an (N,N-disubstituted amino) alkanol alkanoate, a pharmaceutically acceptable salt thereof and a mixture thereof.
- 35. The method of claim 34 wherein the penetration enhancer is dodecyl 2-(N,N-dimethylamino)-propionate or a pharmaceutically acceptable salt.
- 36. The method of claim 22 wherein the lipophilic component comprises at least one aliphatic C8 to C30 ester.
- 37. The method of claim 22 wherein the lipophilic component comprises at least one glyceryl ester selected from the group consisting monoglycerides, diglycerides, triglycerides, and mixtures thereof.
- 38. The method of claim 22 wherein the lipophilic component comprises at least one glyceryl ester selected from the group consisting of glyceryl monooleate, triolein, trimyristin, tristearin, and mixtures thereof.
- 39. The method of claim 22 wherein the composition further comprises an emulsifier selected from the group consisting of sucrose esters, polyoxyethylene sorbitan esters, long chain alcohols, and glyceryl esters.
- 40. The method of claim 22 wherein the emulsifier comprises at least one glyceryl ester selected from the group consisting of glyceryl monooleate, triolein, trimyristin, tristearin, and mixtures thereof.
- 41. The method of claim 22 wherein the composition further comprises up to about 5 percent myrtenol, based on the total weight of the composition.
- 42. The method of claim 22 wherein the composition further comprises a preservative.
- 43. The method of claim 22 wherein the composition further comprises a fragrance.
CROSS REFERENCES TO RELATED APPLICATIONS
[0001] The present application claims the benefit of U.S. Provisional Application No. 60/456,604, filed Mar. 21, 2003 and 60/456,813, filed Mar. 21, 2003. The entire contents of each of the above applications are incorporated herein by reference in their entirety.
Provisional Applications (2)
|
Number |
Date |
Country |
|
60456604 |
Mar 2003 |
US |
|
60456813 |
Mar 2003 |
US |