Details for Patent: 7,442,368

Title:	Delivery of stimulants through an inhalation route
Abstract:	The present invention relates to the delivery of stimulants through an inhalation route. Specifically, it relates to aerosols containing stimulants that are used in inhalation therapy. In a method aspect of the present invention, a stimulant is delivered to a patient through an inhalation route. The method comprises: a) heating a coating of a stimulant, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% stimulant degradation products. In a kit aspect of the present invention, a kit for delivering a stimulant through an inhalation route is provided which comprises: a) a coating of a stimulant drug and b) a device for dispensing said coating a stimulant as a condensation aerosol.
Inventor(s):	Rabinowitz; Joshua D (Mountain View, CA), Zaffaroni; Alejandro C (Atherton, CA)
Assignee:	Alexza Pharmaceuticals, Inc. (Mountain View, CA)
Filing Date:	Mar 07, 2006
Application Number:	11/370,628
Claims:	1. A condensation aerosol for delivery of ephedrine formed by heating a composition containing ephedrine 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 ephedrine and less than 5 percent by weight of ephedrine 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 fenfluramine formed by heating a composition containing fenfluramine 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 fenfluramine and less than 5 percent by weight of fenfluramine 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 method of forming an ephedrine containing aerosol comprising: (a) heating a composition containing ephedrine 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 ephedrine degradation product, and the condensation aerosol has an MMAD of less than 5 microns. 8. The method according to claim 7, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 9. The method according to claim 8, wherein the coated composition comprises at least 10 percent by weight of ephedrine. 10. A method of forming a fenfluramine containing aerosol comprising: (a) heating a composition containing fenfluramine 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 fenfluramine 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 fenfluramine. 13. 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 ephedrine and fenfluramine, 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. 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 the drug. 16. 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 ephedrine and fenfluramine, 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. 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 the salt form of the drug. 19. The condensation aerosol according to claim 2, wherein the condensing comprises allowing the vapor to cool. 20. The condensation aerosol according to claim 5, wherein the condensing comprises allowing the vapor to cool. 21. The method according to claim 8, wherein the condensing comprises allowing the vapor to cool. 22. The method according to claim 11, wherein the condensing comprises allowing the vapor to cool. 23. The method according to claim 14, wherein the condensing comprises allowing the vapor to cool. 24. The method according to claim 17, wherein the condensing comprises allowing the vapor to cool. 25. 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 ephedrine and fenfluramine, 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. 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 condensation aerosol is formed at a rate greater than 0.75 mg/second. 28. The method according to claim 27, wherein the condensation aerosol is formed at a rate greater than 1 mg/second. 29. The method according to claim 28, wherein the condensation aerosol is formed at a rate greater than 2 mg/second. 30. The method according to claim 26, wherein the condensing comprises allowing the vapor to cool.