Delivery of muscle relaxants through an inhalation route
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-009/00
A61K-009/12
A61K-009/14
A61K-031/00
A61K-031/13
A61K-031/135
A61K-031/46
A61K-031/421
A61M-011/00
출원번호
US-0523685
(2006-09-19)
등록번호
US-7507397
(2009-03-24)
발명자
/ 주소
Rabinowitz,Joshua D.
Zaffaroni,Alejandro C.
출원인 / 주소
Alexza Pharmaceuticals, Inc.
대리인 / 주소
Swanson & Bratschun, L.L.C.
인용정보
피인용 횟수 :
18인용 특허 :
144
초록▼
The present invention relates to the delivery of muscle relaxants through an inhalation route. Specifically, it relates to aerosols containing muscle relaxants that are used in inhalation therapy. In a method aspect of the present invention, a muscle relaxant is delivered to a patient through an in
The present invention relates to the delivery of muscle relaxants through an inhalation route. Specifically, it relates to aerosols containing muscle relaxants that are used in inhalation therapy. In a method aspect of the present invention, a muscle relaxant is delivered to a patient through an inhalation route. The method comprises: a) heating a coating of a muscle relaxant, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% muscle relaxant degradation products. In a kit aspect of the present invention, a kit for delivering a muscle relaxant through an inhalation route is provided which comprises: a) a coating of a muscle relaxant and b) a device for dispensing said coating a muscle relaxant as a condensation aerosol.
대표청구항▼
The invention claimed is: 1. A condensation aerosol for delivery of quinine formed by heating a composition containing quinine 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 b
The invention claimed is: 1. A condensation aerosol for delivery of quinine formed by heating a composition containing quinine 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 quinine and less than 5 percent by weight of quinine 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 chlorzoxazone formed by heating a composition containing chlorzoxazone 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 chlorzoxazone and less than 5 percent by weight of chlorzoxazone 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 carisoprodol formed by heating a composition containing carisoprodol 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 carisoprodol and less than 5 percent by weight of carisoprodol 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 condensation aerosol for delivery of cyclobenzaprine formed by heating a composition containing cyclobenzaprine 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 cyclobenzaprine and less than 5 percent by weight of cyclobenzaprine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 11. The condensation aerosol according to claim 10, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 12. The condensation aerosol according to claim 10 or claim 11, wherein the geometric standard deviation around the MMAD is less than 3.0. 13. A method of forming a quinine containing aerosol comprising: (a) heating a composition containing quinine 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 quinine 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 quinine. 16. A method of forming a chlorzoxazone containing aerosol comprising: (a) heating a composition containing chlorzoxazone 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 chlorzoxazone 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 chlorzoxazone. 19. A method of forming a carisoprodol containing aerosol comprising: (a) heating a composition containing carisoprodol 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 carisoprodol 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 carisoprodol. 22. A method of forming a cyclobenzaprine containing aerosol comprising: (a) heating a composition containing cyclobenzaprine 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 cyclobenzaprine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 23. The method according to 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 cyclobenzaprine. 25. 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 quinine, chlorzoxazone, carisoprodol and cyclobenzaprine, and wherein the particles comprise at least 10 percent by weight of the drug and less than 5 percent by weight of the drug quinine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. 26. 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 quinine, chlorzoxazone, carisoprodol, and cyclobenzaprine, 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. 27. The condensation aerosol according to claim 2, wherein the condensing comprises allowing the vapor to cool. 28. The condensation aerosol according to claim 5, wherein the condensing comprises allowing the vapor to cool. 29. The condensation aerosol according to claim 8, wherein the condensing comprises allowing the vapor to cool. 30. The condensation aerosol according to claim 11, wherein the condensing comprises allowing the vapor to cool. 31. The method according to claim 14, wherein the condensing comprises allowing the vapor to cool. 32. The method according to claim 17, wherein the condensing comprises allowing the vapor to cool. 33. The method according to claim 20, wherein the condensing comprises allowing the vapor to cool. 34. The method according to claim 23, wherein the condensing comprises allowing the vapor to cool. 35. The method according to claim 25, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 36. The method according to claim 35, wherein the coated composition comprises at least 10 percent by weight of the drug. 37. The method according to claim 35, wherein the condensing comprises allowing the vapor to cool. 38. The method according to claim 26, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 39. The method according to claim 38, wherein the coated composition comprises at least 10 percent by weight of the salt form of the drug. 40. The method according to claim 38, wherein the condensing comprises allowing the vapor to cool. 41. 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 quinine, chlorzoxazone, carisoprodol, and cyclobenzaprine, 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. 42. The method according to claim 41, wherein the condensation aerosol has an MMAD of 0.2 to 3 microns. 43. The method according to claim 42, wherein the condensation aerosol is formed at a rate greater than 0.75 mg/second. 44. The method according to claim 43, wherein the condensation aerosol is formed at a rate greater than 1 mg/second. 45. The method according to claim 44, wherein the condensation aerosol is formed at a rate greater than 2 mg/second. 46. The method according to claim 42, wherein the condensing comprises allowing the vapor to cool.
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