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Details for Patent: 7,491,047

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Details for Patent: 7,491,047

Title:Delivery of antihistamines through an inhalation route
Abstract: The present invention relates to the delivery of antihistamines through an inhalation route. Specifically, it relates to aerosols containing antihistamines that are used in inhalation therapy. In a method aspect of the present invention, an antihistamine is delivered to a patient through an inhalation route. The method comprises: a) heating a composition, wherein the composition comprises an antihistamine, to form a vapor; and, b) allowing the vapor to cool, thereby forming a condensation aerosol comprising particles with less than 5% antihistamine drug degradation products. In a kit aspect of the present invention, a kit for delivering an antihistamine through an inhalation route is provided which comprises: a) a thin coating of an antihistamine drug composition 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:Aug 22, 2006
Application Number:11/507,986
Claims:1. A condensation aerosol for delivery of azatadine formed by heating a composition containing azatadine 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 azatadine and less than 5 percent by weight of azatadine 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 brompheniramine formed by heating a composition containing brompheniramine 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 brompheniramine and less than 5 percent by weight of brompheniramine 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 between 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 carbinoxamine formed by heating a composition containing carbinoxamine 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 carbinoxamine and less than 5 percent by weight of carbinoxamine 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 chlorpheniramine formed by heating a composition containing chlorpheniramine 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 chlorpheniramine and less than 5 percent by weight of chlorpheniramine 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 clemastine formed by heating a composition containing clemastine 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 clemastine and less than 5 percent by weight of clemastine 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 cyproheptadine formed by heating a composition containing cyproheptadine 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 cyproheptadine and less than 5 percent by weight of cyproheptadine 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 loratadine formed by heating a composition containing loratadine 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 loratadine and less than 5 percent by weight of loratadine 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 pyrilamine formed by heating a composition containing pyrilamine 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 pyrilamine and less than 5 percent by weight of pyrilamine 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 condensation aerosol for delivery of hydroxyzine formed by heating a composition containing hydroxyzine 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 hydroxyzine and less than 5 percent by weight of hydroxyzine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

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

27. The condensation aerosol according to claim 25 or claim 26, wherein the geometric standard deviation around the MMAD is less than 3.0.

28. A condensation aerosol for delivery of promethazine formed by heating a composition containing promethazine 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 promethazine and less than 5 percent by weight of promethazine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

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

30. The condensation aerosol according to claim 28 or claim 29, wherein the geometric standard deviation around the MMAD is less than 3.0.

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

34. A method of forming a brompheniramine containing aerosol comprising: (a) heating a composition containing brompheniramine 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 brompheniramine 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 brompheniramine.

37. A method of forming a carbinoxamine containing aerosol comprising: (a) heating a composition containing carbinoxamine 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 carbinoxamine 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 2.0 to 3 microns.

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

40. A method of forming a chlorpheniramine containing aerosol comprising: (a) heating a composition containing chlorpheniramine 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 chlorpheniramine 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 chlorpheniramine.

43. A method of forming a clemastine containing aerosol comprising: (a) heating a composition containing clemastine 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 clemastine 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 clemastine.

46. A method of forming a cyproheptadine containing aerosol comprising: (a) heating a composition containing cyproheptadine 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 cyproheptadine 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 cyproheptadine.

49. A method of forming a loratadine containing aerosol comprising: (a) heating a composition containing loratadine 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 loratadine 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 loratadine.

52. A method of forming a pyrilamine containing aerosol comprising: (a) heating a composition containing pyrilamine 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 pyrilamine 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 pyrilamine.

55. A method of forming a hydroxyzine containing aerosol comprising: (a) heating a composition containing hydroxyzine 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 hydroxyzine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

56. The method according to claim 55, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

57. The method according to claim 56, wherein the coated composition comprises at least 10 percent by weight of hydroxyzine.

58. A method of forming a promethazine containing aerosol comprising: (a) heating a composition containing promethazine 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 promethazine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

59. The method according to claim 58, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

60. The method according to claim 59, wherein the coated composition comprises at least 10 percent by weight of promethazine.

61. 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 azatadine, brompheniramine, carbinoxamine, chlorpheniramine, clemastine, cyproheptadine, loratadine, pyrilamine, hydroxyzine, and promethazine, 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.

62. The method according to claim 61, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

63. The method according to claim 62, wherein the coated composition comprises at least 10 percent by weight of the drug.

64. 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 azatadine, brompheniramine, carbinoxamine, chlorpheniramine, clemastine, cyproheptadine, loratadine, pyrilamine, hydroxyzine, and promethazine, 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.

65. The method according to claim 64, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

66. The method according to claim 65, wherein the coated composition comprises at least 10 percent by weight of the salt form of the drug.

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

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

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

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

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

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

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

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

75. The condensation aerosol according to claim 26, wherein the condensing comprises allowing the vapor to cool.

76. The condensation aerosol according to claim 29, wherein the condensing comprises allowing the vapor to cool.

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

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

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

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

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

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

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

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

85. The method according to claim 56, wherein the condensing comprises allowing the vapor to cool.

86. The method according to claim 59, wherein the condensing comprises allowing the vapor to cool.

87. The method according to claim 62, wherein the condensing comprises allowing the vapor to cool.

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

89. 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 azatadine, brompheniramine, carbinoxamine, chlorpheniramine, clemastine, cyproheptadine, loratadine, pyrilamine, hydroxyzine, and promethazine, 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.

90. The method according to claim 89, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns.

91. The method according to claim 90, wherein the condensation aerosol is formed at a rate greater than 1 mg/second.

92. The method according to claim 91, wherein the condensation aerosol is formed at a rate greater than 2 mg/second.

93. The method according to claim 89, wherein the condensing comprises allowing the vapor to cool.
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