Delivery of antiemetics through an inhalation route
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-009/12
A61K-009/14
A61M-015/00
출원번호
US-0398383
(2006-04-04)
등록번호
US-7449172
(2008-11-11)
발명자
/ 주소
Rabinowitz,Joshua D
Zaffaroni,Alejandro C
출원인 / 주소
Alexza Pharmaceuticals, Inc.
대리인 / 주소
Swanson & Bratschun, L.L.C.
인용정보
피인용 횟수 :
20인용 특허 :
146
초록▼
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 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.
대표청구항▼
The invention claimed is: 1. A condensation aerosol for delivery of dolasetron formed by heating a composition containing dolasetron coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 per
The invention claimed is: 1. A condensation aerosol for delivery of dolasetron formed by heating a composition containing dolasetron coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of dolasetron and less than 5 percent by weight of dolasetron degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 2. The condensation aerosol according to claim 1, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 3. The condensation aerosol according to claim 1 or claim 2, wherein the geometric standard deviation around the MMAD is less than 3.0. 4. A condensation aerosol for delivery of granisetron formed by heating a composition containing granisetron coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of granisetron and less than 5 percent by weight of granisetron degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 5. The condensation aerosol according to claim 4, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 6. The condensation aerosol according to claim 4 or claim 5, wherein the geometric standard deviation around the MMAD is less than 3.0. 7. A condensation aerosol for delivery of metoclopramide formed by heating a composition containing metoclopramide coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of metoclopramide and less than 5 percent by weight of metoclopramide degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 8. The condensation aerosol according to claim 7, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 9. The condensation aerosol according to claim 7 or claim 8, wherein the geometric standard deviation around the MMAD is less than 3.0. 10. A method of forming a dolasetron containing aerosol comprising: (a) heating a composition containing dolasetron coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of dolasetron degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 11. The method according to claim 10, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 12. The method according to claim 11, wherein the coated composition comprises at least 10 percent by weight of dolasetron. 13. A method of forming a granisetron containing aerosol comprising: (a) heating a composition containing granisetron coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of granisetron degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 14. The method according to claim 13, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 15. The method according to claim 14, wherein the coated composition comprises at least 10 percent by weight of granisetron. 16. A method of forming a metoclopramide containing aerosol comprising: (a) heating a composition containing metoclopramide coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of metoclopramide degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 17. The method according to claim 16, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 18. The method according to claim 17, wherein the coated composition comprises at least 10 percent by weight of metoclopramide. 19. A method of forming a drug containing aerosol comprising: (a) heating a composition containing the drug and a pharmaceutically acceptable excipient coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the drug is selected from the group consisting of dolasetron, granisetron, and metoclopramide, and wherein the particles comprise at least 10 percent by weight of the drug and less than 5 percent by weight of the drug degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 20. The method according to claim 19, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 21. The method according to claim 20, wherein the coated composition comprises at least 10 percent by weight of the drug. 22. A method of forming a drug containing aerosol comprising: (a) heating a composition containing a salt form of the drug coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the drug is selected from the group consisting of dolasetron, granisetron, and metoclopramide, and wherein the particles comprise at least 10 percent by weight of the drug and less than 5 percent by weight of the drug degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 23. The method according to claim 22, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 24. The method according to claim 23, wherein the coated composition comprises at least 10 percent by weight of the salt form of the drug. 25. The condensation aerosol according to claim 2, wherein the condensing comprises allowing the vapor to cool. 26. The condensation aerosol according to claim 5, wherein the condensing comprises allowing the vapor to cool. 27. The condensation aerosol according to claim 8, wherein the condensing comprises allowing the vapor to cool. 28. The method according to claim 11, wherein the condensing comprises allowing the vapor to cool. 29. The method according to claim 14, wherein the condensing comprises allowing the vapor to cool. 30. The method according to claim 17, wherein the condensing comprises allowing the vapor to cool. 31. The method according to claim 20, wherein the condensing comprises allowing the vapor to cool. 32. The method according to claim 23, wherein the condensing comprises allowing the vapor to cool. 33. A method of forming a drug containing aerosol comprising: (a) heating a composition containing the drug coated on a solid support to form a vapor, and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the drug is selected from the group consisting of dolasetron, granisetron, and metoclopramide, wherein the condensation aerosol is formed at a rate greater than 0.5 mg/second, and wherein the particles comprise at least 10 percent by weight of the drug and less than 5 percent by weight of the drug degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 34. The method according to claim 33, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 35. The method according to claim 34, wherein the condensation aerosol is formed at a rate greater than 0.75 mg/second. 36. The method according to claim 35, wherein the condensation aerosol is formed at a rate greater than 1 mg/second. 37. The method according to claim 36, wherein the condensation aerosol is formed at a rate greater than 2 mg/second. 38. The method according to claim 34 wherein the condensing comprises allowing the vapor to cool.
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