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Last Updated: May 4, 2024

Details for Patent: 7,022,312


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Title:Delivery of antiemetics through an inhalation route
Abstract: The present invention relates to the delivery of antiemetics through an inhalation route. Specifically, it relates to aerosols containing antiemetics that are used in inhalation therapy. In a method aspect of the present invention, an antiemetic is delivered to a patient through an inhalation route. The method comprises: a) heating a thin layer of an antiemetic, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% antiemetic degradation products. In a kit aspect of the present invention, a kit for delivering an antiemetic through an inhalation route is provided which comprises: a) a thin layer of an antiemetic drug and b) a device for dispensing said thin layer an antiemetic 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:Mar 31, 2004
Application Number:10/813,721
Claims:1. A condensation aerosol for delivery of a drug selected from the group consisting of dolasetron, granisetron and metoclopramide, 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.10particles per second.

4. A method of producing a drug selected from the group consisting of dolasetron, granisetron and metoclopramide 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.

5. The method according to claim 4, wherein the condensation aerosol is formed at a rate greater than 10.sup.9 particles per second.

6. The method according to claim 5, wherein the condensation aerosol is formed at a rate of greater than 10.sup.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 8, wherein the condensation aerosol is characterized by an MMAD of 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 drug is dolasetron.

14. The condensation aerosol according to claim 1, wherein the drug is granisetron.

15. The condensation aerosol according to claim 1, wherein the drug is metoclopramide.

16. The method according to claim 4, wherein the condensation aerosol is characterized by an MMAD of 0.1 to 5 microns.

17. The method according to claim 4, wherein the condensation aerosol is characterized by an MMAD of less than 3 microns.

18. The method according to claim 17, wherein the condensation aerosol is characterized by an MMAD of about 0.2 to 3 microns.

19. The method according to claim 4, wherein the condensation aerosol is characterized by less than 5% drug degradation products by weight.

20. The method according to claim 19, wherein the condensation aerosol is characterized by less than 2.5% drug degradation products by weight.

21. The method according to claim 4, wherein the solid support is a metal foil.

22. The method according to claim 4, wherein the drug is dolasetron.

23. The method according to claim 4, wherein the drug is granisetron.

24. The method according to claim 4, wherein the drug is metoclopramide.

25. A condensation aerosol for delivery of dolasetron, wherein the condensation aerosol is formed by heating a thin layer containing dolasetron, on a solid support, to produce a vapor of dolasetron, and condensing the vapor to form a condensation aerosol characterized by less than 5% dolasetron degradation products by weight, and an MMAD of about 0.2 to 3 microns.

26. A condensation aerosol for delivery of granisetron, wherein the condensation aerosol is formed by heating a thin layer containing granisetron, on a solid support, to produce a vapor of granisetron, and condensing the vapor to form a condensation aerosol characterized by less than 5% granisetron degradation products by weight, and an MMAD of about 0.2 to 3 microns.

27. A condensation aerosol for delivery of metoclopramide, wherein the condensation aerosol is formed by heating a thin layer containing metoclopramide, on a solid support, to produce a vapor of metoclopramide, and condensing the vapor to form a condensation aerosol characterized by less than 5% metoclopramide degradation products by weight, and an MMAD of about 0.2 to 3 microns.

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

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

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

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