Details for Patent: 7,449,174

Title:	Delivery of analgesics through an inhalation route
Abstract:	The present invention relates to the delivery of analgesics through an inhalation route. Specifically, it relates to aerosols containing acetaminophen, orphenadrine or tramadol that are used in inhalation therapy. In a method aspect of the present invention, an analgesic is administered to a patient through an inhalation route. The method comprises: a) heating a thin layer of acetaminophen, orphenadrine or tramadol, on a solid support to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% acetaminophen, orphenadrine or tramadol degradation products. In a kit aspect of the present invention, a kit for delivering acetaminophen, orphenadrine or tramadol through an inhalation is provided which comprises: a) a thin coating of an acetaminophen, orphenadrine or tramadol 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:	Jun 30, 2006
Application Number:	11/479,892
Claims:	1. A condensation aerosol for delivery of acetaminophen formed by heating a composition containing acetaminophen 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 acetaminophen and less than 5 percent by weight of acetaminophen 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 orphenadrine formed by heating a composition containing orphenadrine 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 orphenadrine and less than 5 percent by weight of orphenadrine degradation products, andthe 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 tramadol formed by heating a composition containing tramadol 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 tramadol and less than 5 percent by weight of tramadol 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 method of forming an acetaminophen containing aerosol comprising: (a) heating a composition containing acetaminophen 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 acetaminophen 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 acetaminophen. 13. A method of forming an orphenadrine containing aerosol comprising: (a) heating a composition containing orphenadrine 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 orphenadrine 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 orphenadrine. 16. A method of forming a tramadol containing aerosol comprising: (a) heating a composition containing tramadol 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 tramadol 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 tramadol. 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 acetaminophen, orphenadrine, and tramadol, 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 acetaminophen, orphenadrine, and tramadol, 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 acetaminophen, orphenadrine, and tramadol, 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 33 wherein the condensing comprises allowing the vapor to cool.