Delivery of antiemetics through an inhalation route
View Patent ↗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.
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 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 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 9 particles per second.
6. The method according to claim 5 , wherein the condensation aerosol is formed at a rate of 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 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.