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Details for Patent: 7,052,680

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Details for Patent: 7,052,680

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 dispending 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:10/816,567
Claims:1. A condensation aerosol for delivery of a drug selected from the group consisting of benzotropine, pergolide, amantadine, deprenyl and ropinerole, 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 condensation aerosol according to claim 1, wherein the condensation aerosol is formed at a rate greater than 10.sup.9 particles per second.

3. The condensation aerosol according to claim 2, wherein the condensation aerosol is formed at a rate greater than 10.sup.10 particles per second.

4. The condensation aerosol according to claim 1, wherein the condensation aerosol is characterized by less than 2.5% drug degradation products by weight.

5. A method of producing a drug selected from the group consisting of benzotropine, pergolide, amantadine, deprenyl and ropinerole in an aerosol form comprising: a. heating a thin layer containing the drug, on a solid support, to produce a vapor of the drug, and b. providing an air flow through 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.

6. The method according to claim 5, wherein the condensation aerosol is formed at a rate greater than 10.sup.9 particles per second.

7. The method according to claim 6, wherein the condensation aerosol is formed at a rate greater than 10.sup.10 particles per second.

8. The condensation aerosol according to claim 1, wherein the condensation aerosol is characterized by an MMAD of 0.1 to 5 microns.

9. The condensation aerosol according to claim 1, wherein the condensation aerosol is characterized by an MMAD of less than 3 microns.

10. The condensation aerosol according to claim 1, wherein the condensation aerosol is characterized by an MMAD of about 0.2 to about 3 microns.

11. The condensation aerosol according to claim 1, wherein the condensation aerosol is characterized by less than 5% drug degradation products by weight.

12. The condensation aerosol according to claim 1, wherein the thin layer contains at least 80% drug by weight.

13. The condensation aerosol according to claim 12, wherein the thin layer contains at least 95% drug by weight.

14. The condensation aerosol according to claim 1, wherein the condensation aerosol comprises at least 80% drug by weight.

15. The condensation aerosol according to claim 14, wherein the condensation aerosol comprises at least 95% drug by weight.

16. The condensation aerosol according to claim 1, wherein the thin layer has a thickness between 0.004 and 3 microns.

17. The condensation aerosol according to claim 1, wherein the solid support has the surface texture of a metal foil.

18. The condensation aerosol according to claim 1, wherein the solid support is a metal foil.

19. The condensation aerosol according to claim 1, wherein the drug is benzotropine.

20. The condensation aerosol according to claim 1, wherein the drug is pergolide.

21. The method according to claim 5, wherein the condensation aerosol is characterized by an MMAD of about 0.2 to 3 microns.

22. The condensation aerosol according to claim 1, wherein the drug is deprenyl.

23. The condensation aerosol according to claim 1, wherein the drug is ropinerole.

24. The method according to claim 5, wherein the condensation aerosol is characterized by an MMAD of 0.1 to 5 microns.

25. The method according to claim 5, wherein the condensation aerosol is characterized by an MMAD of less than 3 microns.

26. The method according to claim 25, wherein the condensation aerosol is characterized by an MMAD of about 0.2 to about 3 microns.

27. The method according to claim 5, wherein the condensation aerosol is characterized by less than 5% drug degradation products by weight.

28. The method according to claim 27, wherein the condensation aerosol is characterized by less than 2.5% drug degradation products by weight.

29. The method according to claim 5, wherein the thin layer contains at least 80% drug by weight.

30. The method according to claim 29, wherein the thin layer contains at least 95% drug by weight.

31. The method according to claim 5, wherein the condensation aerosol comprises at least 80% drug by weight.

32. The method according to claim 31, wherein the condensation aerosol comprises at least 95% drug by weight.

33. The method according to claim 5, wherein the thin layer has a thickness between 0.004 and 3 microns.

34. The method according to claim 5, wherein the solid support has the surface texture of a metal foil.

35. The method according to claim 5, wherein the solid support is a metal foil.

36. A method of producing benzotropine in an aerosol form comprising: a. heating a thin layer containing benzotropine, on a solid support, to produce a vapor of benzotropine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% benzotropine degradation products by weight, and an MMAD of about 0.2 and about 3 microns.

37. A method of producing pergolide in an aerosol form comprising: a. heating a thin layer containing pergolide, on a solid support, to produce a vapor of pergolide, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% pergolide degradation products by weightm and an MMAD of about 0.2 and about 3 microns.

38. A method of producing amantadine in an aerosol form comprising: a. heating a thin layer containing amantadine, on a solid support, to produce a vapor of amantadine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% amantadine degradation products by weight, and an MMAD of about 0.2 and about 3 microns.

39. A method of producing deprenyl in an aerosol form comprising: a. heating a thin layer containing deprenyl, on a solid support, to produce a vapor of deprenyl, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% deprenyl degradation products by weight, and an MMAD of about 0.2 and about 3 microns.

40. A method of producing ropinerole in an aerosol form comprising: a. heating a thin layer containing ropinerole, on a solid support, to produce a vapor of ropinerole, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% ropinerole degradation products by weight, and an MMAD of about 0.2 and about 3 microns.
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