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Details for Patent: 7,507,398

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Details for Patent: 7,507,398

Title:Delivery of physiologically active compounds through an inhalation route
Abstract: The present invention relates to the delivery of physiologically active compounds through an inhalation route. Specifically, it relates to aerosols containing physiologically active compounds that are used in inhalation therapy. In a method aspect of the present invention, the physiologically active compound is delivered to a patient through an inhalation route. The method comprises: a) heating a coating of a physiologically active compound, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% physiologically active compound degradation products. In a kit aspect of the present invention, a kit for delivering a physiologically active compound through an inhalation route is provided which comprises: a) a thin coating of a physiologically active compound, and b) a device for dispensing said thin coating as a condensation aerosol.
Inventor(s): Rabinowitz; Joshua D (Princeton, NJ), Zaffaroni; Alejandro C (Atherton, CA)
Assignee: Alexza Pharmaceuticals, Inc. (Mountain View, CA)
Filing Date:Jun 30, 2006
Application Number:11/479,509
Claims:1. A condensation aerosol for delivery of chlordiazepoxide formed by heating a composition containing chlordiazepoxide coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of chlordiazepoxide and less than 5 percent by weight of chlordiazepoxide degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

2. The condensation aerosol according to claim 1, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

3. The condensation aerosol according to claim 1 or claim 2, wherein the geometric standard deviation around the MMAD is less than 3.0.

4. A condensation aerosol for delivery of betahistine formed by heating a composition containing betahistine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of betahistine and less than 5 percent by weight of betahistine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

5. The condensation aerosol according to claim 4, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

6. The condensation aerosol according to claim 4 or claim 5, wherein the geometric standard deviation around the MMAD is less than 3.0.

7. A condensation aerosol for delivery of clonidine formed by heating a composition containing clonidine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of clonidine and less than 5 percent by weight of clonidine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

8. The condensation aerosol according to claim 7, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

9. The condensation aerosol according to claim 7 or claim 8, wherein the geometric standard deviation around the MMAD is less than 3.0.

10. A condensation aerosol for delivery of testosterone formed by heating a composition containing testosterone coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of testosterone and less than 5 percent by weight of testosterone degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

11. The condensation aerosol according to claim 10, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

12. The condensation aerosol according to claim 10 or claim 11, wherein the geometric standard deviation around the MMAD is less than 3.0.

13. A condensation aerosol for delivery of a conjugated estrogen formed by heating a composition containing the conjugated estrogen coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of the conjugated estrogen and less than 5 percent by weight of the conjugated estrogen degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

14. The condensation aerosol according to claim 13, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

15. The condensation aerosol according to claim 13 or claim 14, wherein the geometric standard deviation around the MMAD is less than 3.0.

16. A condensation aerosol for delivery of estradiol formed by heating a composition containing estradiol coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of estradiol and less than 5 percent by weight of estradiol degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

17. The condensation aerosol according to claim 16, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

18. The condensation aerosol according to claim 16 or claim 17, wherein the geometric standard deviation around the MMAD is less than 3.0.

19. A condensation aerosol for delivery of ethinyl estradiol formed by heating a composition containing ethinyl estradiol coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of ethinyl estradiol and less than 5 percent by weight of ethinyl estradiol degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

20. The condensation aerosol according to claim 19, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

21. The condensation aerosol according to claim 19 or claim 20, wherein the geometric standard deviation around the MMAD is less than 3.0.

22. A condensation aerosol for delivery of hyoscyamine formed by heating a composition containing hyoscyamine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of hyoscyamine and less than 5 percent by weight of hyoscyamine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

23. The condensation aerosol according to claim 22, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

24. The condensation aerosol according to claim 22 or claim 23, wherein the geometric standard deviation around the MMAD is less than 3.0.

25. A method of forming a chlordiazepoxide containing aerosol comprising: (a) heating a composition containing chlordiazepoxide coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of chlordiazepoxide degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

26. The method according to claim 25, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

27. The method according to claim 26, wherein the coated composition comprises at least 10 percent by weight of chlordiazepoxide.

28. A method of forming a betahistine containing aerosol comprising: (a) heating a composition containing betahistine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of betahistine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

29. The method according to claim 28, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

30. The method according to claim 29, wherein the coated composition comprises at least 10 percent by weight of betahistine.

31. A method of forming a clonidine containing aerosol comprising: (a) heating a composition containing clonidine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of clonidine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

32. The method according to claim 31, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

33. The method according to claim 32, wherein the coated composition comprises at least 10 percent by weight of clonidine.

34. A method of forming a testosterone containing aerosol comprising: (a) heating a composition containing testosterone coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of testosterone degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

35. The method according to claim 34, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

36. The method according to claim 35, wherein the coated composition comprises at least 10 percent by weight of testosterone.

37. A method of forming a conjugated estrogen containing aerosol comprising: (a) heating a composition containing the conjugated estrogen coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of the conjugated estrogen degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

38. The method according to claim 37, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

39. The method according to claim 38, wherein the coated composition comprises at least 10 percent by weight of the conjugated estrogen.

40. A method of forming an estradiol containing aerosol comprising: (a) heating a composition containing estradiol coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of estradiol degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

41. The method according to claim 40, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

42. The method according to claim 41, wherein the coated composition comprises at least 10 percent by weight of estradiol.

43. A method of forming an ethinyl estradiol containing aerosol comprising: (a) heating a composition containing ethinyl estradiol coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of ethinyl estradiol degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

44. The method according to claim 43, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

45. The method according to claim 44, wherein the coated composition comprises at least 10 percent by weight of ethinyl estradiol.

46. A method of forming a hyoscyamine containing aerosol comprising: (a) heating a composition containing hyoscyamine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of hyoscyamine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

47. The method according to claim 46, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

48. The method according to claim 47, wherein the coated composition comprises at least 10 percent by weight of hyoscyamine.

49. A method of forming a drug containing aerosol comprising: (a) heating a composition containing the drug and a pharmaceutically acceptable excipient coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the drug is selected from the group consisting of chlordiazepoxide, betahistine, clonidine, testosterone, conjugated estrogens, estradiol, ethinyl estradiol, and hyoscyamine, and wherein the particles comprise at least 10 percent by weight of the drug and less than 5 percent by weight of the drug degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

50. The method according to claim 49, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

51. The method according to claim 50, wherein the coated composition comprises at least 10 percent by weight of the drug.

52. A method of forming a drug containing aerosol comprising: (a) heating a composition containing a salt form of the drug coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the drug is selected from the group consisting of chlordiazepoxide, betahistine, clonidine, testosterone, conjugated estrogens, estradiol, ethinyl estradiol, and hyoscyamine, and wherein the particles comprise at least 10 percent by weight of the drug and less than 5 percent by weight of the drug degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

53. The method according to claim 52, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

54. The method according to claim 53, wherein the coated composition comprises at least 10 percent by weight of the salt form of the drug.

55. The condensation aerosol according to claim 2, wherein the condensing comprises allowing the vapor to cool.

56. The condensation aerosol according to claim 5, wherein the condensing comprises allowing the vapor to cool.

57. The condensation aerosol according to claim 8, wherein the condensing comprises allowing the vapor to cool.

58. The condensation aerosol according to claim 11, wherein the condensing comprises allowing the vapor to cool.

59. The condensation aerosol according to claim 14, wherein the condensing comprises allowing the vapor to cool.

60. The condensation aerosol according to claim 17, wherein the condensing comprises allowing the vapor to cool.

61. The condensation aerosol according to claim 20, wherein the condensing comprises allowing the vapor to cool.

62. The condensation aerosol according to claim 23, wherein the condensing comprises allowing the vapor to cool.

63. The method according to claim 26, wherein the condensing comprises allowing the vapor to cool.

64. The method according to claim 29, wherein the condensing comprises allowing the vapor to cool.

65. The method according to claim 32, wherein the condensing comprises allowing the vapor to cool.

66. The method according to claim 35, wherein the condensing comprises allowing the vapor to cool.

67. The method according to claim 38, wherein the condensing comprises allowing the vapor to cool.

68. The method according to claim 41, wherein the condensing comprises allowing the vapor to cool.

69. The method according to claim 44, wherein the condensing comprises allowing the vapor to cool.

70. The method according to claim 47, wherein the condensing comprises allowing the vapor to cool.

71. The method according to claim 50, wherein the condensing comprises allowing the vapor to cool.

72. The method according to claim 53, wherein the condensing comprises allowing the vapor to cool.

73. A method of forming a drug containing aerosol comprising: (a) heating a composition containing the drug coated on a solid support to form a vapor, and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the drug is selected from the group consisting of chlordiazepoxide, betahistine, clonidine, testosterone, conjugated estrogens, estradiol, ethinyl estradiol, and hyoscyamine, wherein the condensation aerosol is formed at a rate greater than 0.5 mg/second, and wherein the particles comprise at least 10 percent by weight of the drug and less than 5 percent by weight of the drug degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

74. The method according to claim 73, wherein the condensation aerosol is formed at a rate greater than 1 mg/second.

75. The method according to claim 74, wherein the condensation aerosol is formed at a rate greater than 2 mg/second.

76. The method according to claim 75, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

77. The method according to claim 74, wherein the condensing comprises allowing the vapor to cool.
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