Details for Patent: 7,465,436

Title:	Delivery of compounds for the treatment of Parkinson's through an inhalation route
Abstract:	The present invention relates to the delivery of antiparkinsons drugs through an inhalation route. In a method aspect of the present invention, an antiparkinsons drug is administered to a patient through an inhalation route. The method comprises: a) heating a thin layer of an antiparkinsons drug on a solid support to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% drug degradation products. In a kit aspect of the present invention, a kit for delivering an antiparkinsons drug through an inhalation route is provided which comprises: a) a thin coating of a an antiparkinsons drug composition; and, b) a device for dispending 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:	May 30, 2006
Application Number:	11/442,917
Claims:	1. A condensation aerosol for delivery of benzotropine formed by heating a composition containing benzotropine 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 benzotropine and less than 5 percent by weight of benzotropine 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 pergolide formed by heating a composition containing pergolide 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 pergolide and less than 5 percent by weight of pergolide 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 amantadine formed by heating a composition containing amantadine 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 amantadine and less than 5 percent by weight of amantadine 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 deprenyl formed by heating a composition containing deprenyl 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 deprenyl and less than 5 percent by weight of deprenyl 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 ropinerole formed by heating a composition containing ropinerole 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 ropinerole and less than 5 percent by weight of ropinerole 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 method of forming a benzotropine containing aerosol comprising: (a) heating a composition containing benzotropine 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 benzotropine 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 benzotropine. 19. A method of forming a pergolide containing aerosol comprising: (a) heating a composition containing pergolide 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 pergolide 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 pergolide. 22. A method of forming an amantadine containing aerosol comprising: (a) heating a composition containing amantadine 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 amantadine 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 amantadine. 25. A method of forming a deprenyl containing aerosol comprising: (a) heating a composition containing deprenyl 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 deprenyl 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 coated composition comprises at least 10 percent by weight of deprenyl. 28. A method of forming a ropinerole containing aerosol comprising: (a) heating a composition containing ropinerole 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 ropinerole degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 29. The method according to claim 28, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 30. The method according to claim 29, wherein the coated composition comprises at least 10 percent by weight of ropinerole. 31. 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 benzotropine, pergolide, amantadine, deprenyl, and ropinerole, 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. 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 the drug. 34. 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 benzotropine, pergolide, amantadine, deprenyl, and ropinerole, 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. 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 the salt form of the drug. 37. The condensation aerosol according to claim 2, wherein the condensing comprises allowing the vapor to cool. 38. The condensation aerosol according to claim 5, wherein the condensing comprises allowing the vapor to cool. 39. The condensation aerosol according to claim 8, wherein the condensing comprises allowing the vapor to cool. 40. The condensation aerosol according to claim 11, wherein the condensing comprises allowing the vapor to cool. 41. The condensation aerosol according to claim 14, wherein the condensing comprises allowing the vapor to cool. 42. The method according to claim 17, wherein the condensing comprises allowing the vapor to cool. 43. The method according to claim 20, wherein the condensing comprises allowing the vapor to cool. 44. The method according to claim 23, wherein the condensing comprises allowing the vapor to cool. 45. The method according to claim 26, wherein the condensing comprises allowing the vapor to cool. 46. The method according to claim 29, wherein the condensing comprises allowing the vapor to cool. 47. The method according to claim 32, wherein the condensing comprises allowing the vapor to cool. 48. The method according to claim 35, wherein the condensing comprises allowing the vapor to cool. 49. 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 benzotropine, pergolide, amantadine, deprenyl, and ropinerole, 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. 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 condensation aerosol is formed at a rate greater than 0.75 mg/second. 52. The method according to claim 51, wherein the condensation aerosol is formed at a rate greater than 1 mg/second. 53. The method according to claim 52, wherein the condensation aerosol is formed at a rate greater than 2 mg/second. 54. The method according to claim 49, wherein the condensing comprises allowing the vapor to cool.