Details for Patent: 7,011,820

Title:	Delivery of compounds for the treatment of Parkinsons 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 dispensing said thin coating as a condensation aerosol.
Inventor(s):	Rabinowitz; Joshua D. (Mountain View, CA), Zaffaroni; Alejandro C. (Atherton, CA)
Assignee:	Alexza Pharmaceuticals, Inc. (Palo Alto, CA)
Filing Date:	Apr 01, 2004
Application Number:	10/816,407
Claims:	1. A method of treating Parkinsons disease in a patient comprising administering a therapeutic amount of a drug condensation aerosol to the patient by inhalation, wherein the drug is selected from the group consisting of benzotropine, pergolide, ropinerole, amantadine and deprenyl, and wherein the condensation aerosol is formed by heating a thin layer containing the drug, on a solid support, to produce a vapor of the drug, and condensing the vapor to form a condensation aerosol characterized by less than 10% drug degradation products by weight, and an MMAD of less than 5 microns. 2. The method according to claim 1, wherein the condensation aerosol is characterized by an MMAD of less than 3 microns. 3. The method according to claim 1, wherein the condensation aerosol is formed at a rate greater than 0.5 mg/second. 4. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.1 mg and 4 mg of benzotropine delivered in a single inspiration. 5. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.01 mg and 2.5 mg of pergolide delivered in a single inspiration. 6. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.02 mg and 4 mg of ropinerole delivered in a single inspiration. 7. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 5 mg and 500 mg of anamtadine delivered in a single inspiration. 8. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.5 mg and 12.5 mg of deprenyl delivered in a single inspiration. 9. The method according to claim 1, wherein peak plasma drug concentration is reached in less than 0.1 hours. 10. The method according to claim 1, wherein at least 50% by weight of the condensation aerosol is amorphous in form. 11. A method of administering a drug condensation aerosol to a patient comprising administering the drug condensation aersol to the patient by inhalation, wherein the drug is selected from the group consisting of benzotropine, pergolide, ropinerole, amantadine and deprenyl, and wherein the drug condensation aerosol is formed by heating a thin layer containing the drug, on a solid support, to produce a vapor of the drug, and condensing the vapor to form a condensation aerosol characterized by less than 10% drug degradation products by weight, and an MMAD of less than 5 microns. 12. A kit for delivering a drug condensation aerosol comprising: a. a thin layer containing the drug, on a solid support, wherein the drug is selected from the group consisting of benzotropine, pergolide, ropinerole, amantadine and deprenyl, and b. a device for providing the condensation aerosol, wherein the condensation aerosol is formed by heating the thin layer to produce a vapor of the drug, and condensing the vapor to form a condensation aerosol characterized by less than 10% drug degradation products by weight, and an MMAD of less than 5 microns. 13. The kit according to claim 12, wherein the device comprises: a. a flow through enclosure containing the solid support, b. a power source that can be activated to heat the solid support, and c. at least one portal through which air can be drawn by inhalation, wherein activation of the power source is effective to produce a vapor of the drug, and drawing air through the enclosure is effective to condense the vapor to form the condensation aerosol. 14. The kit according to claim 13, wherein the heat for heating the solid support is generated by an exothermic chemical reaction. 15. The kit according to claim 14, wherein the exothermic chemical reaction is oxidation of combustible materials. 16. The kit according to claim 13, wherein the heat for heating the solid support is generated by passage of current through an electrical resistance element. 17. The kit according to claim 13, wherein the solid support has a surface area dimensioned to accommodate a therapeutic dose of the drug. 18. The kit according to claim 12, wherein peak plasma drug concentration is reached in less than 0.1 hours. 19. The kit according to claim 12, further including instructions for use. 20. The method according to claim 1, wherein the condensation aerosol is characterized by an MMAD of 0.2 to 5 microns. 21. The method according to claim 2, wherein the condensation aerosol is characterized by an MMAD of 0.2 to 3 microns. 22. The method according to claim 1, wherein the thin layer has a thickness between 0.004 and 3 microns. 23. The method according to claim 11, wherein the drug is benzotropine. 24. The method according to claim 11, wherein the drug is pergolide. 25. The method according to claim 11, wherein the drug is ropinerole. 26. The method according to claim 11, wherein the drug is amantadine. 27. The method according to claim 11, wherein the drug is deprenyl. 28. The kit according to claim 12, wherein the condensation aerosol is characterized by an MMAD of less than 3 microns. 29. The kit according to claim 12, wherein the condensation aerosol is characterized by an MMAD of 0.2 to 5 microns. 30. The kit according to claim 32, wherein the condensation aerosol is characterized by an MMAD of 0.2 to 3 microns. 31. The kit according to claim 12, wherein the thin layer has a thickness between 0.004 and 3 microns. 32. The kit according to claim 12, wherein the drug is benzotropine. 33. The kit according to claim 12, wherein the drug is pergolide. 34. The kit according to claim 12, wherein the drug is ropinerole. 35. The kit according to claim 12, wherein the drug is amantadine. 36. The kit according to claim 12, wherein the drug is deprenyl. 37. The kit according to claim 13, wherein the solid support has a surface to mass ratio of greater than 1 cm.sup.2 per gram. 38. The kit according to claim 13, wherein the solid support has a surface to volume ratio of greater than 100 per meter. 39. The kit according to claim 13, wherein the solid support is a metal foil. 40. The kit according to claim 39, wherein the metal foil has a thickness of less than 0.25 mm.