Details for Patent: 7,524,484

Title:	Delivery of diphenhydramine through an inhalation route
Abstract:	The present invention relates to the delivery of diphenhydramine through an inhalation route. In a composition aspect of the present invention, a composition of a diphenhydramine condensation aerosol is presented. In a method aspect of the present invention, diphenhydramine aerosol is formed by: a) heating a thin layer of diphenhydramine on a solid support to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% degradation product and an aerosol having an MMAD less than 3 microns. In a kit aspect of the present invention, a kit for delivering a condensation aerosol is provided which comprises: a) a thin coating of diphenhydramine; and b) a device for dispensing the diphenhydramine as an 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:	11/479,361
Claims:	1. A condensation aerosol for delivery of diphenhydramine formed by heating a composition containing diphenhydramine 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 diphenhydramine and less than 5 percent by weight of diphenhydramine 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 method of forming a diphenhydramine containing aerosol comprising: (a) heating a composition containing diphenhydramine 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 diphenhydramine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 5. The method according to claim 4, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 6. The method according to claim 5, wherein the coated composition comprises at least 10 percent by weight of diphenhydramine. 7. A method of forming a diphenhydramine containing aerosol comprising: (a) heating a composition containing diphenhydramine and a pharmaceutically acceptable 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 at least 10 percent by weight of diphenhydramine and less than 5 percent by weight of diphenhydramine degradation products, 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 diphenhydramine. 10. A method of forming a diphenhydramine containing aerosol comprising: (a) heating a composition containing a salt form of diphenhydramine 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 at least 10 percent by weight of diphenhydramine and less than 5 percent by weight of diphenhydramine 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 the salt form of diphenhydramine. 13. The condensation aerosol according to claim 2, wherein the condensing comprises allowing the vapor to cool. 14. The method according to claim 5, wherein the condensing comprises allowing the vapor to cool. 15. The method according to claim 8, wherein the condensing comprises allowing the vapor to cool. 16. The method according to claim 11, wherein the condensing comprises allowing the vapor to cool. 17. A method of forming a diphenhydramine containing aerosol comprising: (a) heating a composition containing diphenhydramine coated on a solid support to form a vapor, and (b) condensing the vapor to form a condensation aerosol comprising particles, 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 diphenhydramine and less than 5 percent by weight of diphenhydramine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 18. The method according to claim 17, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 19. The method according to claim 18, wherein the condensation aerosol is formed at a rate greater than 1 mg/second. 20. The method according to claim 19, wherein the condensation aerosol is formed at a rate greater than 2 mg/second. 21. The method according to claim 17, wherein the condensing comprises allowing the vapor to cool.