Delivery of anti-migraine compounds 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-0768220
(2004-01-29)
발명자
/ 주소
Rabinowitz,Joshua D.
Zaffaroni,Alejandro C.
출원인 / 주소
Alexza Pharmaceuticals, Inc.
대리인 / 주소
Swanson &
인용정보
피인용 횟수 :
48인용 특허 :
78
초록▼
The present invention relates to the delivery of anti-migraine compounds through an inhalation route. Specifically, it relates to aerosols containing lidocaine, verapamil, diltiazem, isometheptene, or lisuride that are used in inhalation therapy. In a method aspect of the present invention, lidocain
The present invention relates to the delivery of anti-migraine compounds through an inhalation route. Specifically, it relates to aerosols containing lidocaine, verapamil, diltiazem, isometheptene, or lisuride that are used in inhalation therapy. In a method aspect of the present invention, lidocaine, verapamil, diltiazem, isometheptene, or lisuride is administered to a patient through an inhalation route. The method comprises: a) heating a thin layer of lidocaine, verapamil, diltiazem, isometheptene, or lisuride, 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 lidocaine, verapamil, diltiazem, isometheptene, or lisuride through an inhalation route is provided which comprises: a) a thin coating of a lidocaine, verapamil, diltiazem, isometheptene, or lisuride composition and b) a device for dispensing said thin coating as a condensation aerosol.
대표청구항▼
The invention claimed is: 1. A condensation aerosol for delivery of a drug selected from the group consisting of lidocaine, verapamil, diltiazem, isometheptene and lisuride, wherein the condensation aerosol is formed by heating a thin layer containing the drug, on a solid support, to produce a vapo
The invention claimed is: 1. A condensation aerosol for delivery of a drug selected from the group consisting of lidocaine, verapamil, diltiazem, isometheptene and lisuride, 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 109 particles per second. 3. The condensation aerosol according to claim 2, wherein the condensation aerosol is formed at a rate greater than 1010 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 lidocaine, verapamil, diltiazem, isometheptene and lisuride 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 109 particles per second. 7. The method according to claim 6, wherein the condensation aerosol is formed at a rate greater than 1010 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 9, wherein the condensation aerosol is characterized by an MMAD of about 0.2 and 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 solid support is a metal foil. 13. The condensation aerosol according to claim 1, wherein the drug is lidocaine. 14. The condensation aerosol according to claim 1, wherein the drug is verapamil. 15. The condensation aerosol according to claim 1, wherein the drug is diltiazem. 16. The condensation aerosol according to claim 1, wherein the drug is isometheptene. 17. The condensation aerosol according to claim 1, wherein the drug is lisuride. 18. The method according to claim 5, wherein the condensation aerosol is characterized by an MMAD of 0.1 to 5 microns. 19. The method according to claim 5, wherein the condensation aerosol is characterized by an MMAD of less than 3 microns. 20. The method according to claim 5, wherein the condensation aerosol is characterized by an MMAD of about 0.2 to about 3 microns. 21. The method according to claim 5, wherein the condensation aerosol is characterized by less than 5% drug degradation products by weight. 22. The method according to claim 21, wherein the condensation aerosol is characterized by less than 2.5% drug degradation products by weight. 23. The method according to claim 5, wherein the solid support is a metal foil. 24. The method according to claim 5, wherein the drug is lidocaine. 25. The method according to claim 5, wherein the drug is verapamil. 26. The method according to claim 5, wherein the drug is diltiazem. 27. The method according to claim 5, wherein the drug is isometheptene. 28. The method according to claim 5, wherein the drug is lisuride. 29. A condensation aerosol for delivery of lidocaine, wherein the condensation aerosol is formed by heating a thin layer containing lidocaine, on a solid support, to produce a vapor of lidocaine, and condensing the vapor to form a condensation aerosol characterized by less than 5% lidocaine degradation products by weight, and an MMAD of about 0. 2 to 3 microns. 30. A condensation aerosol for delivery of verapamil, wherein the condensation aerosol is formed by heating a thin layer containing verapamil, on a solid support, to produce a vapor of verapamil, and condensing the vapor to form a condensation aerosol characterized by less than 5% verapamil degradation products by weight, and an MMAD of about 0. 2 to 3 microns. 31. A condensation aerosol for delivery of diltiazem, wherein the condensation aerosol is formed by heating a thin layer containing diltiazem, on a solid support, to produce a vapor of diltiazem, and condensing the vapor to form a condensation aerosol characterized by less than 5% diltiazem degradation products by weight, and an MMAD of about 0. 2 to 3 microns. 32. A condensation aerosol for delivery of isometheptene, wherein the condensation aerosol is formed by heating a thin layer containing isometheptene, on a solid support, to produce a vapor of isometheptene, and condensing the vapor to form a condensation aerosol characterized by less than 5% isometheptene degradation products by weight, and an MMAD of about 0.2 to 3 microns. 33. A condensation aerosol for delivery of lisuride, wherein the condensation aerosol is formed by heating a thin layer containing lisuride, on a solid support, to produce a vapor of lisuride, and condensing the vapor to form a condensation aerosol characterized by less than 5% lisuride degradation products by weight, and an MMAD of about 0.2 to 3 microns. 34. A method of producing lidocaine in an aerosol form comprising: a. heating a thin layer containing lidocaine, on a solid support, to produce a vapor of lidocaine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% lidocaine degradation products by weight, and an MMAD of about 0.2 to about 3 microns. 35. A method of producing verapamil in an aerosol form comprising: a. heating a thin layer containing verapamil, on a solid support, to produce a vapor of verapamil, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% verapamil degradation products by weight, and an MMAD of about 0.2 to about 3 microns. 36. A method of producing diltiazem in an aerosol form comprising: a. heating a thin layer containing diltiazem, on a solid support, to produce a vapor of diltiazem, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% diltiazem degradation products by weight, and an MMAD of about 0.2 to about 3 microns. 37. A method of producing isometheptene in an aerosol form comprising: a. heating a thin layer containing isometheptene, on a solid support, to produce a vapor of isometheptene, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% isometheptene degradation products by weight, and an MMAD of about 0.2 to about 3 microns. 38. A method of producing lisuride in an aerosol form comprising: a. heating a thin layer containing lisuride, on a solid support, to produce a vapor of lisuride, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% lisuride degradation products by weight, and an MMAD of about 0.2 to about 3 microns.
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