Delivery of sedative-hypnotics through an inhalation route
View Patent ↗The present invention relates to the delivery of sedative-hypnotics through an inhalation route. Specifically, it relates to aerosols containing sedative-hypnotics that are used in inhalation therapy. In a method aspect of the present invention, a sedative-hypnotic drug is administered to a patient through an inhalation route. The method comprises: a) heating a thin layer of a sedative-hypnotic, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% sedative-hypnotic drug degradation products. In a kit aspect of the present invention, a kit for delivering a sedative-hypnotic through an inhalation route is provided which comprises: a) a thin layer of a sedative-hypnotic drug and b) a device for dispensing said thin layer a sedative-hypnotic drug as a condensation aerosol.
1. A condensation aerosol for delivery of a drug selected from the group consisting of zaleplon, zolpidem and zopiclone, 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. A method of producing a drug selected from the group consisting of zaleplon, zolpidem and zopiclone 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, and an MMAD of less than 5 microns.
5. The method according to claim 4 , wherein the condensation aerosol is formed at a rate greater than 10 9 particles per second.
6. The method according to claim 5 , wherein the condensation aerosol is formed at a rate greater than 10 10 particles per second.
7. The condensation aerosol according to claim 1 , wherein the condensation aerosol is characterized by an MMAD of 0.1 to 5 microns.
8. The condensation aerosol according to claim 1 , wherein the condensation aerosol is characterized by an MMAD of less than 3 microns.
9. The condensation aerosol according to claim 7 , wherein the condensation aerosol is characterized by an MMAD of about 0.2 to 3 microns.
10. The condensation aerosol according to claim 1 , wherein the condensation aerosol is characterized by less than 5% drug degradation products by weight.
11. The condensation aerosol according to claim 10 , wherein the condensation aerosol is characterized by less than 2.5% drug degradation products by weight.
12. The condensation aerosol according to claim 1 , wherein the solid support is a metal foil.
13. The condensation aerosol according to claim 1 , wherein the thin layer has a thickness between 1.5 and 4.4 microns.
14. The condensation aerosol according to claim 1 , wherein the drug is zaleplon.
15. The condensation aerosol according to claim 1 , wherein the drug is zolpidem.
16. The condensation aerosol according to claim 1 , wherein the drug is zopiclone.
17. The method according to claim 4 , wherein the condensation aerosol is characterized by an MMAD of 0.1 to 5 microns.
18. The method according to claim 4 , wherein the condensation aerosol is characterized by an MMAD of less than 3 microns.
19. The method according to claim 4 , wherein the condensation aerosol is characterized by an MMAD of about 0.2 to 3 microns.
20. The method according to claim 4 , wherein the condensation aerosol is characterized by less than 5% drug degradation products by weight.
21. The method according to claim 20 , wherein the condensation aerosol is characterized by less than 2.5% drug degradation products by weight.
22. The method according to claim 4 , wherein the solid support is a metal foil.
23. The method according to claim 1 , wherein the thin layer has a thickness between 1.5 and 4.4 microns.
24. The method according to claim 4 , wherein the drug is zaleplon.
25. The method according to claim 4 , wherein the drug is zolpidem.
26. The method according to claim 4 , wherein the drug is zopiclone.
27. A condensation aerosol for delivery of zaleplon, wherein the condensation aerosol is formed by heating a thin layer containing zaleplon, on a solid support, to produce a vapor of zaleplon, and condensing the vapor to form a condensation aerosol characterized by less than 5% zaleplon degradation products by weight, and an MMAD of about 0.2 to 3 microns.
28. A condensation aerosol for delivery of zolpidem, wherein the condensation aerosol is formed by heating a thin layer containing zolpidem, on a solid support, to produce a vapor of zolpidem, and condensing the vapor to form a condensation aerosol characterized by less than 5% zolpidem degradation products by weight, and an MMAD of about 0.2 to 3 microns.
29. A condensation aerosol for delivery of zopiclone, wherein the condensation aerosol is formed by heating a thin layer containing zopiclone, on a solid support, to produce a vapor of zopiclone, and condensing the vapor to form a condensation aerosol characterized by less than 5% zopiclone degradation products by weight, and an MMAD of about 0.2 to 3 microns.
30. A method of producing zaleplon in an aerosol form comprising:
a. heating a thin layer containing zaleplon, on a solid support, to produce a vapor of zaleplon, and
b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% zaleplon degradation products by weight, and an MMAD of about 0.2 to 3 microns.
31. A method of producing zolpidem in an aerosol form comprising:
a. heating a thin layer containing zolpidem, on a solid support, to produce a vapor of zolpidem, and
b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% zolpidem degradation products by weight, and an MMAD of about 0.2 to 3 microns.
32. A method of producing zopiclone in an aerosol form comprising:
a. heating a thin layer containing zopiclone, on a solid support, to produce a vapor of zopiclone, and
b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% zopiclone degradation products by weight, and an MMAD of about 0.2 to 3 microns.