Delivery of compounds for the treatment of Parkinsons through an inhalation route
View Patent ↗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.
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 9 particles per second.
3. The condensation aerosol according to claim 2 , wherein the condensation aerosol is formed at a rate greater than 10 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 9 particles per second.
7. The method according to claim 6 , wherein the condensation aerosol is formed at a rate greater than 10 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.