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Claims for Patent: 8,784,882

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Claims for Patent: 8,784,882

Title:Controlled release delivery system for nasal applications and method of treatment
Abstract: This invention relates to a gel formulation for nasal administration of a controlled release formulation of hormones to the systemic circulation and/or to the brain. The special lipophilic or partly lipophilic system of the invention leads to higher bioavailability of the active ingredient caused by sustained serum levels in plasma but also leads to a more favorable serum level profile. The special lipophilic or partly lipophilic system also allows for the modulation of brain functioning. The invention also relates to the nasal administration of steroid hormones for treatment of female sexual dysfunction (FSD) or female arousal disorder.
Inventor(s): Mattern; Claudia (Stans, CH)
Assignee: Mattern Pharma AG (Vaduz, LI)
Application Number:13/194,853
Patent Claims: 1. A method of testosterone replacement therapy comprising the step of nasally administering to a patient in need of such treatment an effective amount of a testosterone gel formulation comprising a) testosterone; b) at least one lipophilic or partly lipophilic carrier; and c) a compound or a mixture of compounds having surface tension decreasing activity.

2. A method according to claim 1, wherein said lipophilic carrier comprises an oil.

3. A method according to claim 2, wherein said oil is a vegetable oil.

4. A method according to claim 3, wherein said vegetable oil is castor oil.

5. A method according to claim 4, wherein the castor oil is hydrogenated.

6. A method according to claim 3, wherein said vegetable oil is soybean oil.

7. A method according to claim 3, wherein said vegetable oil is sesame oil.

8. A testosterone gel formulation according to claim 3, wherein said vegetable oil is peanut oil.

9. A method according to claim 2, wherein said lipophilic carrier comprises an oil mixture.

10. A method according to claim 2, wherein the oil is present in an amount from about 30% to about 98% by weight of the testosterone gel formulation.

11. A method according to claim 1, wherein said lipophilic carrier comprises a fatty acid ester.

12. A method according to claim 11, wherein the fatty acid ester is ethyloleat.

13. A method according to claim 11, where the fatty acid ester is oleyloleat.

14. A method according to claim 1, wherein said lipophilic carrier comprises isopropylmyrisate.

15. A method according to claim 1, wherein said lipophilic carrier comprises medium chain triglycerides.

16. A method according to claim 1, wherein said lipophilic carrier comprises glycerol esters of fatty acids.

17. A method according to claim 1, wherein said lipophilic carrier comprises polyethylene glycol.

18. A method according to claim 1, wherein said lipophilic carrier comprises phospholipids.

19. A method according to claim 1, wherein said lipophilic carrier comprises white soft paraffin.

20. A method according to claim 1, wherein said compound or a mixture of compounds having surface tension decreasing activity comprise (a) at least one surfactant selected from the group consisting of lecithin, a fatty acid ester and mixtures thereof, (b) at least one humectant selected from the group consisting of sorbitol, glycerine, polyethylene glycol and a macrogol glycerol fatty acid ester and mixtures thereof, and (c) mixtures thereof.

21. A method according to claim 1, wherein said compound or a mixture of compounds having surface tension decreasing activity comprises an oleoyl macrogolglyceride or a mixture of oleoyl macrogolglycerides.

22. A method according to claim 20, wherein said compound or a mixture of compounds having surface tension decreasing activity is present within the testosterone gel formulation in an amount of from about 1% to about 20% by weight of the testosterone gel formulation.

23. A method according to claim 1, further comprising a viscosity regulating agent.

24. A method according to claim 23, wherein said viscosity regulating agent comprises a thickener or gelling agent selected from the group consisting of cellulose and cellulose derivatives, polysaccharides, carbomers, polyvinyl alcohol, povidone, colloidal silicon dioxide, cetyl alcohols, stearic acid, beeswax, petrolatum, triglycerides, lanolin and mixtures thereof.

25. A method according to claim 23, wherein said viscosity regulating agent is colloidal silicon dioxide.

26. A method according to claim 23, wherein the viscosity regulating agent is present within the testosterone gel formulation in an amount of from about 0.5% to about 10% by weight of the testosterone gel formulation.

27. A method according to claim 1, wherein said testosterone is present within the testosterone gel formulation in an amount of from about 0.2% to about 6% by weight, of the testosterone gel formulation.

28. A method according to claim 1, wherein said testosterone is introduced into the testosterone gel formulation as microparticles.

29. A method according to claim 1, wherein said testosterone is introduced into the testosterone gel formulation as nanoparticles.

30. A method according to claim 1, wherein said testosterone is introduced into the testosterone gel formulation as liposomes.

31. A method according to claim 1, wherein said testosterone is introduced into the testosterone gel formulation as bilayer vesicles.

32. A method according to claim 1, wherein said testosterone is introduced into the testosterone gel formulation as micelles.

33. A method according to claim 1, wherein testosterone gel formulation provides for the controlled release of said testosterone into the systemic circulation after nasal application.

34. A method according to claim 33, wherein the testosterone gel formulation provides for sustained serum levels of said testosterone.

35. A method according to claim 33, wherein said testosterone is maintained at a serum level greater than baseline for at least 6 hours following nasal administration.

36. A method according to claim 35, wherein the testosterone serum level is achieved after one application per nostril of the testosterone gel formulation.

37. A method according to claim 35, wherein the level of unbound testosterone is similar to the physiologic daily rhythm of testosterone release.

38. A method according to claim 37, wherein the level of unbound testosterone is constant for at least about 6 hours following nasal administration.

39. A method according to claim 1, wherein the testosterone gel formulation is provided in a device capable of delivering multiple, individual doses of the testosterone gel formulation.

40. A method according to claim 2, wherein the oil is present in an amount of from about 60% to about 98% by weight of the testosterone gel formulation.

41. A method according to claim 2, wherein the oil is present in an amount of from about 75% to about 95% by weight of the testosterone gel formulation.

42. A method according to claim 2, wherein the oil is present in an amount of from about 85% to about 95% by weight of the testosterone gel formulation.

43. A method according to claim 2, wherein the oil is present in an amount of about 90% by weight of the testosterone gel formulation.

44. A method according to claim 20, wherein said compound or a mixture of compounds having surface tension decreasing activity is present within the testosterone gel formulation in an amount of from about 1% to about 10% by weight of the testosterone gel formulation.

45. A method according to claim 20, wherein said compound or a mixture of compounds having surface tension decreasing activity is present within the testosterone gel formulation in an amount of from about 1% to about 5% by weight of the testosterone gel formulation.

46. A method according to claim 20, wherein said compound or a mixture of compounds having surface tension decreasing activity is present within the testosterone gel formulation in an amount of about 4% by weight of the testosterone gel formulation.

47. A method according to claim 23, wherein the viscosity regulating agent is present within the testosterone gel formulation in an amount of from about 0.5% to about 7% by weight of the testosterone gel formulation.

48. A method according to claim 23, wherein the viscosity regulating agent is present within the testosterone gel formulation in an amount of from about 1% to about 4% by weight of the testosterone gel formulation.

49. A method according to claim 23, wherein the viscosity regulating agent is present within the testosterone gel formulation in an amount of about 4% by weight of the testosterone gel formulation.

50. A method according to claim 33, wherein said testosterone is maintained at a serum level greater than baseline for at least about 8 hours following nasal administration.

51. A method according to claim 33, wherein said testosterone is maintained at a serum level greater than baseline for at least about 10 hours following nasal administration.

52. A method according to claim 37, wherein the level of unbound testosterone is constant for at least about 8 hours following nasal administration.

53. A method according to claim 37, wherein the level of unbound testosterone is constant for at least about 10 hours following nasal administration.

54. A method of testosterone replacement therapy comprising the step of nasally administering to a patient in need of such treatment an effective amount of a testosterone gel formulation comprising a) testosterone; b) at least one lipophilic or partly lipophilic carrier in an amount from about 60% to about 98% by weight of the testosterone gel formulation; c) a compound or a mixture of compounds having surface tension decreasing activity in an amount from about 1% to about 20% by weight of the testosterone gel formulation; and d) a viscosity regulating agent in an amount from about 0.5% to about 10% by weight of the testosterone gel formulation.

55. A method of testosterone replacement therapy comprising the step of nasally administering to a patient in need of such treatment an effective amount of a testosterone gel formulation comprising a) testosterone; b) castor oil in an amount from about 60% to about 98% by weight of the testosterone gel formulation; c) an oleoyl macrogolglyceride or a mixture of oleoyl macrogolglycerides in an amount from about 1% to about 20% by weight of the testosterone gel formulation; and d) colloidal silicone dioxide in an amount from about 0.5% to about 10% by weight of the testosterone gel formulation.
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