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Claims for Patent: 5,023,252

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Claims for Patent: 5,023,252

Title: Transdermal and trans-membrane delivery of drugs
Abstract:The rate of absorption of drugs across skin and other body membranes such as mucous membranes and the blood brain barrier is enhanced by adding to the drug composition a compound which enhances the rate. This compound may be macrocyclic ester, diester, amide, diamide, amidine, diamidine, thioester, dithioester, thioamide, ketone or lactone. The macrocyclic ketone contains at least 12 carbon atoms.
Inventor(s): Hseih; Dean (Brandamore, PA)
Assignee: Conrex Pharmaceutical Corporation (Malvern, PA)
Application Number:07/449,117
Patent Claims: 1. A method for increasing the rate of passage of a drug across animal or human skin, mucous membranes, or the blood brain barrier which comprises applying to the skin, mucous membrane or blood brain barrier a composition comprising an effective amount of the drug, a pharmaceutical carrier, and from about 0.1 to about 50% by weight of a compound (with or without dissolving in a solvent) effecting such increase in rate, said compound having the structure: ##STR6## wherein X and Y are oxygen, sulfur or an imino group of the structure ##STR7## or .dbd.N--R, with the proviso that when Y is an imino group, X is an imino group, and when Y is sulfur, X is sulfur or an imino group, A is a group having the structure ##STR8## wherein X and Y are as defined above, m and n are integers having a value from 1 to 20 and the sum of m+n is not greater than 25, p is an integer having a value of 0 or 1, q is an integer having a value of 0 or 1, r is an integer having a value of 0 or 1, and each of R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 is independently hydrogen or an alkyl group having from 1 to 6 carbon atoms which may be straight chained or branched, provided that only one of R.sub.1 to R.sub.6 can be alkyl group, with the proviso that when p, q and r are 0 and Y is oxygen, then m+n is at least 11, and with the further proviso that when X is an imino group, q is equal to 1, Y is oxygen, and p and r are 0, then m+n is at least 11.

2. A method according to claim 1 wherein the amount of compound effecting the increase in the rate of passage is from about 0.1 to 30% by weight.

3. A method according to claim 1 wherein Y is sulfur, X is sulfur or imino, and A is ##STR9##

4. A method according to claim 1 wherein Y is imino, X is sulfur or imino, and A is ##STR10##

5. A method according to claim 1 wherein r is 0.

6. A method according to claim 5 wherein Y is sulfur and X is sulfur or imino.

7. A method according to claim 5 wherein Y is imino and X is imino.

8. A method according to claim 5 wherein Y is oxygen and X is sulfur or imino.

9. A method according to claim 1 wherein the R on the imino is lower alkyl.

10. A method according to claim 1 wherein the compound has the structure ##STR11## ##STR12## Wherein A is a carbo-oxy group of the structure ##STR13##

11. A method according to claim 10 wherein the amount of compound effecting the increase in the rate of passage is from about 0.1 to 30% by weight.

12. A method according to claim 10 wherein q and r are 1.

13. A method according to claim 12 wherein p is 0.

14. A method according to claim 13 wherein m+n is at least 3.

15. A method according to claim 10 wherein q is 1 and r is 0.

16. A method according to claim 15 wherein p is 0.

17. A method according to claim 10 wherein p, q and r are 0.

18. A method according to claim 17 wherein m+n is 11 to 15.

19. A method according to claim 18 wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are hydrogen.

20. A method according to claim 18 wherein one of R.sub.1, R.sub.2, R.sub.3, or R.sub.4 is lower alkyl.

21. A method according to claim 20 wherein one of R.sub.1, R.sub.2, R.sub.3, or R.sub.4 is methyl.

22. A method according to claim 19 wherein m+n is 11.

23. A method according to claim 19 wherein m+n is 14.

24. A method according to claim 21 wherein m+n is 14.

25. A method according to claim 10 wherein r is 0, q and p are 1, m is 7 and n is 7.

26. A method according to claim 10 wherein q is 1, and r are 0 and m+n is 15.

27. A method according to claim 17 wherein the concentration of the compound is at least 2%.

28. A composition for administering a drug across skin, mucous membranes or blood brain barrier which contains an effective amount of a drug, a pharmaceutical carrier, and from about 0.1% to about 50% by weight of a compound (with or without dissolving in a solvent) which increases the rate of passage of the drug across the skin, the mucous membranes, or the blood brain barrier, said compound having the structure: ##STR14## wherein X and Y are oxygen, sulfur or an imino group of the structure ##STR15## or .dbd.N--R, with the proviso that when Y is an imino group, X is an imino group, and when Y is sulfur, X is sulfur or an imino group, A is a group having the structure ##STR16## wherein X and Y are as defined above, m and n are integers having a value from 1 to 20 and the sum of m+n is not greater than 25, p is an integer having a value of 0 or 1, q is an integer having a value of 0 or 1, r is an integer having a value of 0 or 1, and each of R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 is independently hydrogen or an alkyl group having from 1 to 6 carbon atoms which may be straight chained or branched, provided that only one of R.sub.1 to R.sub.6 can be alkyl group, with the proviso that when p, q and r are 0 and Y is oxygen, then m+n is at least 11, and with the further proviso that when X is an imino group, q is equal to 1, Y is oxygen, and p and r are 0, then m+n is at least 11.

29. A composition according to claim 28 wherein each of X and Y is oxygen and wherein A is a carbo-oxy group of the structure ##STR17##

30. A composition according to claim 29 wherein q and r are 1.

31. A composition according to claim 30 wherein p is 0.

32. A composition according to claim 30 wherein m+n is at least 3.

33. A composition according to claim 29 wherein q is 1 and r is 0.

34. A composition according to claim 33 wherein p is 0.

35. A composition according to claim 29 wherein p, q and r are 0.

36. A composition according to claim 35 wherein m+n is 11 to 15.

37. A composition according to claim 36 wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are hydrogen.

38. A composition according to claim 36 wherein one of R.sub.1, R.sub.2, R.sub.3, or R.sub.4 is lower alkyl.

39. A composition according to claim 38 wherein one of R.sub.1, R.sub.2, R.sub.3, or R.sub.4 is methyl.

40. A composition according to claim 37 wherein m+n is 11.

41. A composition according to claim 37 wherein m+n is 14.

42. A composition according to claim 39 wherein m+n is 14.

43. A composition according to claim 29 wherein r is 0, p and q are 1, m is 7 and n is 7.

44. A composition according to claim 29 wherein q is 1, p and r are 0, and m+n is 15.

45. A composition according to claim 35 wherein the concentration of the compound is at least 2%.

46. A composition according to claim 44 wherein the concentration of the compound is at least 0.5%.

47. A composition according to claim 29 which is the form of a lotion.

48. A composition according to claim 29 which is the form of a cream.

49. A composition according to claim 29 which is the form of a film.

50. A composition according to claim 29 which is the form of a dermal patch.

51. A composition according to claim 29 which is the form of a solution.

52. A composition according to claim 29 which is the form of a spray solution.

53. A composition according to claim 51 wherein the composition is held in a sponge.
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