Details for Patent: 7,445,768

Title:	Delivery of sedative-hypnotics through an inhalation route
Abstract:	The present invention relates to the delivery of sedative-hypnotics through an inhalation route. Specifically, it relates to aerosols containing sedative-hypnotics that are used in inhalation therapy. In a method aspect of the present invention, a sedative-hypnotic drug is administered to a patient through an inhalation route. The method comprises: a) heating a thin layer of a sedative-hypnotic, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% sedative-hypnotic drug degradation products. In a kit aspect of the present invention, a kit for delivering a sedative-hypnotic through an inhalation route is provided which comprises: a) a thin layer of a sedative-hypnotic drug and b) a device for dispensing said thin layer a sedative-hypnotic drug 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 07, 2006
Application Number:	11/500,735
Claims:	1. A condensation aerosol for delivery of zaleplon formed by heating a composition containing zaleplon 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 zaleplon and less than 5 percent by weight of zaleplon 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 zolpidem formed by heating a composition containing zolpidem 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 zolpidem and less than 5 percent by weight of zolpidem 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 zopiclone formed by heating a composition containing zopiclone 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 zopiclone and less than 5 percent by weight of zopiclone degradation products, and the condensation aerosol has an MMAD between 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 method of forming a zaleplon containing aerosol comprising: (a) heating a composition containing zaleplon 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 zaleplon degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 11. The method according to claim 10, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 12. The method according to claim 11, wherein the coated composition comprises at least 10 percent by weight of zaleplon. 13. A method of forming a zolpidem containing aerosol comprising: (a) heating a composition containing zolpidem 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 zolpidem degradation product, and the condensation aerosol has an MMAD of less than 5 microns. 14. The method according to claim 13, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 15. The method according to claim 14, wherein the coated composition comprises at least 10 percent by weight of zolpidem. 16. A method of forming a zopiclone containing aerosol comprising: (a) heating a composition containing zopiclone 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 zopiclone degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 17. The method according to claim 16, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 18. The method according to claim 17, wherein the coated composition comprises at least 10 percent by weight of zopiclone. 19. 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 zaleplon, zolpidem, and zopiclone, 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. 20. The method according to claim 19, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 21. The method according to claim 20, wherein the coated composition comprises at least 10 percent by weight of the drug. 22. 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 zaleplon, zolpidem, and zopiclone, 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. 23. The method according to claim 22, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 24. The method according to claim 23, wherein the coated composition comprises at least 10 percent by weight of the salt form of the drug. 25. The condensation aerosol according to claim 2, wherein the condensing comprises allowing the vapor to cool. 26. The condensation aerosol according to claim 5, wherein the condensing comprises allowing the vapor to cool. 27. The condensation aerosol according to claim 8, wherein the condensing comprises allowing the vapor to cool. 28. The method according to claim 11, wherein the condensing comprises allowing the vapor to cool. 29. The method according to claim 14, wherein the condensing comprises allowing the vapor to cool. 30. The method according to claim 17, wherein the condensing comprises allowing the vapor to cool. 31. The method according to claim 20, wherein the condensing comprises allowing the vapor to cool. 32. The method according to claim 23, wherein the condensing comprises allowing the vapor to cool. 33. 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 zaleplon, zolpidem, and zopiclone, 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. 34. The method according to claim 33, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 35. The method according to claim 34, wherein the condensation aerosol is formed at a rate greater than 0.75 mg/second. 36. The method according to claim 35, wherein the condensation aerosol is formed at a rate greater than 1 mg/second. 37. The method according to claim 36, wherein the condensation aerosol is formed at a rate greater than 2 mg/second. 38. The method according to claim 34, wherein the condensing comprises allowing the vapor to cool.