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Claims for Patent: 4,863,970

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Claims for Patent: 4,863,970

Title: Penetration enhancement with binary system of oleic acid, oleins, and oleyl alcohol with lower alcohols
Abstract:Penetration-enhancing pharmaceutical compositions for topical transepidermal and percutaneous application are disclosed which are non-irritating to the skin. These compositions are made up of a safe and effective amount of an active pharmaceutical permeant, including hydrophilic salt forms, contained in a novel penetration-enhancing vehicle comprising, (i) 1-95% w. of a cell-envelope disordering compound selected from the group consisting of oleic acid, oleyl alcohol, glycerol monoleate, glycerol dioleate, glycerol trioleate and mixtures thereof, (ii) 5-75% w., and preferably 5-49% w., of a lower alkanol selected from the group consisting of ethanol, propanol and isopropanol and mixtures thereof and (iii) 0-45% w., and preferably 1-45% w., of an inert diluent which, according to properties of the permeant used, may range from hydrophilic to hydrophobic. Water, polyethylene or polypropylene glycols and mineral oil are exemplary diluents.
Inventor(s): Patel; Dinesh C. (Murray, UT), Chang; Yunik (Lakewood, NJ)
Assignee: Theratech, Inc. (Salt Lake City, UT)
Application Number:07/218,702
Patent Claims: 1. A pharmaceutical composition for topical application having penetration-enhancing properties consisting essentially of:

(a) a safe and effective amount of an active pharmaceutical agent contained in,

(b) a penetration-enhancing vehicle exclusive of diols and N-cyclic solvents consisting essentially of:

(i) 1-95% by weight of one or more cell-envelope disordering compounds selected from the group consisting of oleic acid, oleyl alcohol, glycerol esters of oleic acid and mixtures thereof;

(ii) 5-75% by weight of a lower alkanol selected from the group consisting of ethanol, propanol and isopropanol and mixtures thereof; and

(iii) 0-45% by weight of an inert diluent.

2. A composition according to claim 1 wherein the lower alkanol is present in amounts of between 5 and 49% by weight.

3. A composition according to claim 2 wherein the active pharmaceutical agent is present in amount ranging from about 0.01 to 50% by weight and the penetration enhancing vehicle is present in amounts ranging from about 50-99.99% by weight.

4. A composition according to claim 3 wherein the cell-envelope disordering compounds are members selected from the following groupings:

(1) oleic acid and oleyl alcohol or mixtures thereof;

(2) one or more glycerol esters of oleic acid;

(3) oleic acid and one or more glycerol esters of oleic acid;

(4) oleyl alcohol and one or more glycerols ester of oleic acid; and

(5) mixtures of oleic acid and oleyl alcohol and one or more glycerol esters of oleic acid.

5. A composition according to claim 4 wherein the active pharmaceutical agent is present in amounts ranging from about 0.01 to 30% by weight and the penetration enhancing vehicle is present in amounts ranging from about 70 to 99.99% by weight.

6. A composition according to claim 5 wherein the cell-envelope disordering compound is a member selected from the group consisting of oleic acid and oleyl alcohol and mixtures thereof.

7. A composition according to claim 5 wherein the cell-envelope disordering compound is oleic acid.

8. A composition according to claim 6 wherein the cell-envelope disordering compound is oleyl alcohol.

9. A composition according to claim 5 wherein the cell-envelope disordering compound is a member selected from the group consisting of a one or more glycerol esters of oleic acid.

10. A composition according to claim 9 wherein the cell-envelope disordering compound is glycerol monooleate.

11. A composition according to claim 8 wherein the cell-envelope disordering compound is glycerol dioleate.

12. A composition according to claim 7 wherein the cell-envelope disordering compound is glycerol trioleate.

13. A composition according to claim 5 wherein the cell-envelope disordering compound is oleic acid admixed with a member selected from the group consisting of a one or more glycerol esters of oleic acid.

14. A composition according to claim 13 wherein the cell-envelope disordering compound is glycerol monooleate.

15. A composition according to claim 13 wherein the cell-envelope disordering compound is glycerol dioleate.

16. A composition according to claim 13 wherein the cell-envelope disordering compound is glycerol trioleate.

17. A composition according to claim 5 wherein the cell-envelope disordering compound is oleyl alcohol admixed with a member selected from the group consisting of a one or more glycerol esters of oleic acid.

18. A composition according to claim 17 wherein the cell-envelope disordering compound is glycerol monooleate.

19. A composition according to claim 17 wherein the cell-envelope disordering compound is glycerol dioleate.

20. A composition according to claim 17 wherein the cell-envelope disordering compound is glycerol trioleate.

21. A composition according to claim 5 wherein the alcohol is present in the penetration enhancer vehicle in amounts of between about 20 and 49% by weight.

22. A composition according to claim 4 wherein the inert diluent is present in the penetration enhancer vehicle in amounts ranging from 1 to 45% by weight.

23. A composition according to claim 22 wherein the active pharmaceutical agent is present in amounts ranging from about 0.01 to 30% by weight and the penetration enhancing is present in amounts ranging from about 70 to 99.99% by weight.

24. A composition according to claim 23 wherein the cell-envelope disordering compound is a member selected from the group consisting of oleic acid and oleyl alcohol and mixtures thereof.

25. A composition according to claim 24 wherein the cell-envelope disordering compound is oleic acid.

26. A composition according to claim 24 wherein the cell-envelope disordering compound is oleyl alcohol.

27. A method according to claim 23 wherein the cell-envelope disordering compound is a member selected from the group consisting of a one or more glycerol esters of oleic acid.

28. A composition according to claim 27 wherein the cell-envelope disordering compound is glycerol monooleate.

29. A composition according to claim 27 wherein the cell-envelope disordering compound is glycerol dioleate.

30. A composition according to claim 27 wherein the cell-envelope disordering compound is glycerol trioleate.

31. A composition according to claim 23 wherein the cell-envelope disordering compound is oleic acid admixed with a member selected from the group consisting of a one or more glycerol esters of oleic acid.

32. A composition according to claim 31 wherein the cell-envelope disordering compound is glycerol monooleate.

33. A composition according to claim 31 wherein the cell-envelope disordering compound is glycerol dioleate.

34. A composition according to claim 31 wherein the cell-envelope disordering compound is glycerol trioleate.

35. A composition according to claim 23 wherein the cell-envelope disordering compound is oleyl alcohol admixed with a member selected from the group consisting of a one or more glycerol esters of oleic acid.

36. A composition according to claim 35 wherein the cell-envelope disordering compound is glycerol monooleate.

37. A composition according to claim 35 wherein the cell-envelope disordering compound is glycerol dioleate.

38. A composition according to claim 35 wherein the cell-envelope disordering compound is glycerol trioleate.

39. A composition according to claim 23 wherein the inert diluent is a member selected from the group consisting of water, polypropylene glycol, polyethylene glycol, polyvinyl alcohols, polyvinylpyrrolidone, mineral oil, silicone oil, ethylene-vinyl acteate polymers or other suitable water or oil soluble low molecular weight polymers.

40. A composition according to claim 23 wherein the alcohol is present in the penetration enhancer combination in amounts between about 20 and 49% by weight.
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