Delivery of opioids 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-0768281
(2004-01-29)
발명자
/ 주소
Rabinowitz,Joshua D.
Zaffaroni,Alejandro C.
출원인 / 주소
Alexza Pharmaceuticals, Inc.
대리인 / 주소
Swanson & Bratschun, L.L.C.
인용정보
피인용 횟수 :
72인용 특허 :
81
초록▼
The present invention relates to the delivery of opioids through an inhalation route. Specifically, it relates to aerosols containing opioids that are used in inhalation therapy. In a method aspect of the present invention, an opioid is delivered to a patient through an inhalation route. The method
The present invention relates to the delivery of opioids through an inhalation route. Specifically, it relates to aerosols containing opioids that are used in inhalation therapy. In a method aspect of the present invention, an opioid is delivered to a patient through an inhalation route. The method comprises: a) heating a thin layer of an opioid, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% opioid degradation products. In a kit aspect of the present invention, a kit for delivering an opioid through an inhalation route is provided which comprises: a) a thin layer of an opioid and b) a device for dispensing said thin layer as a condensation aerosol.
대표청구항▼
The invention claimed is: 1. A condensation aerosol for delivery of a drug selected from the group consisting of naltrexone, buprenorphine, naloxone, butorphanol, hydromorphone, oxycodone, methadone, remifentanil, sufentanil, nalbuphine and fentanyl wherein the condensation aerosol is formed by hea
The invention claimed is: 1. A condensation aerosol for delivery of a drug selected from the group consisting of naltrexone, buprenorphine, naloxone, butorphanol, hydromorphone, oxycodone, methadone, remifentanil, sufentanil, nalbuphine and fentanyl 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. A method of producing a drug selected from the group consisting of naltrexone, buprenorphine, naloxone, butorphanol, hydromorphone, oxycodone, methadone, remifentanil, sufentanil, nalbuphine and fentanyl 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 109 particles per second. 6. The method according to claim 5, wherein the condensation aerosol is formed at a rate greater than 1010 particles per second. 7. The condensation aerosol according to claim 1, wherein the condensation aerosol is characterized by an MMAD of 0.2 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 claim 1, 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 naltrexone. 14. The condensation aerosol according to claim 1, wherein the drug is buprenorphine. 15. The condensation aerosol according to claim 1, wherein the drug is naloxone. 16. The condensation aerosol according to claim 1, wherein the drug is butorphanol. 17. The condensation aerosol according to claim 1, wherein the drug is hydromorphone. 18. The condensation aerosol according to claim 1, wherein the drug is oxycodone. 19. The condensation aerosol according to claim 1, wherein the drug is methadone. 20. The condensation aerosol according to claim 1, wherein the drug is remifentanil. 21. The condensation aerosol according to claim 1, wherein the drug is sufentanil. 22. The condensation aerosol according to claim 1, wherein the drug is nalbuphine. 23. The condensation aerosol according to claim 1, wherein the drug is fentanyl. 24. The method according to claim 4, wherein the condensation aerosol is characterized by an MMAD of 0.2 to 5 microns. 25. The method according to claim 4, wherein the condensation aerosol is characterized by an MMAD of less than 3 microns. 26. The method according to claim 4, wherein the condensation aerosol is characterized by an MMAD of 0.2 to 3 microns. 27. The method according to claim 4, wherein the condensation aerosol is characterized by less than 5% drug degradation products by weight. 28. The method according to claim 27, wherein the condensation aerosol is characterized by less than 2.5% drug degradation products by weight. 29. The method according to claim 4, wherein the solid support is a metal foil. 30. The method according to claim 4, wherein the drug is naltrexone. 31. The method according to claim 4, wherein the drug is buprenorphine. 32. The method according to claim 4, wherein the drug is naloxone. 33. The method according to claim 4, wherein the drug is butorphanol. 34. The method according to claim 4, wherein the drug is hydromorphone. 35. The method according to claim 4, wherein the drug is oxycodone. 36. The method according to claim 4, wherein the drug is methadone. 37. The method according to claim 4, wherein the drug is remifentanil. 38. The method according to claim 4, wherein the drug is sufentanil. 39. The method according to claim 4, wherein the drug is nalbuphine. 40. The method according to claim 4, wherein the drug is fentanyl. 41. A condensation aerosol for delivery of naltrexone, wherein the condensation aerosol is formed by heating a thin layer containing naltrexone, on a solid support, to produce a vapor of naltrexone, and condensing the vapor to form a condensation aerosol characterized by less than 5% naltrexone degradation products by weight, and an MMAD of 0.2 to 3 microns. 42. A condensation aerosol for delivery of buprenorphine, wherein the condensation aerosol is formed by heating a thin layer containing buprenorphine, on a solid support, to produce a vapor of buprenorphine, and condensing the vapor to form a condensation aerosol characterized by less than 5% buprenorphine degradation products by weight, and an MMAD of 0.2 to 3 microns. 43. A condensation aerosol for delivery of naloxone, wherein the condensation aerosol is formed by heating a thin layer containing naloxone, on a solid support, to produce a vapor of naloxone, and condensing the vapor to form a condensation aerosol characterized by less than 5% naloxone degradation products by weight, and an MMAD of 0.2 to 3 microns. 44. A condensation aerosol for delivery of butorphanol, wherein the condensation aerosol is formed by heating a thin layer containing butorphanol, on a solid support, to produce a vapor of butorphanol, and condensing the vapor to form a condensation aerosol characterized by less than 5% butorphanol degradation products by weight, and an MMAD of 0.2 to 3 microns. 45. A condensation aerosol for delivery of hydromorphone, wherein the condensation aerosol is formed by heating a thin layer containing hydromorphone, on a solid support, to produce a vapor of hydromorphone, and condensing the vapor to form a condensation aerosol characterized by less than 5% hydromorphone degradation products by weight, and an MMAD of 0.2 to 3 microns. 46. A condensation aerosol for delivery of oxycodone, wherein the condensation aerosol is formed by heating a thin layer containing oxycodone, on a solid support, to produce a vapor of oxycodone, and condensing the vapor to form a condensation aerosol characterized by less than 5% oxycodone degradation products by weight, and an MMAD of 0.2 to 3 microns. 47. A condensation aerosol for delivery of methadone, wherein the condensation aerosol is formed by heating a thin layer containing methadone, on a solid support, to produce a vapor of methadone, and condensing the vapor to form a condensation aerosol characterized by less than 5% methadone degradation products by weight, and an MMAD of 0.2 to 3 microns. 48. A condensation aerosol for delivery of remifentanil, wherein the condensation aerosol is formed by heating a thin layer containing remifentanil, on a solid support, to produce a vapor of remifentanil, and condensing the vapor to form a condensation aerosol characterized by less than 5% remifentanil degradation products by weight, and an MMAD of 0.2 to 3 microns. 49. A condensation aerosol for delivery of sufentanil, wherein the condensation aerosol is formed by heating a thin layer containing sufentanil, on a solid support, to produce a vapor of sufentanil, and condensing the vapor to form a condensation aerosol characterized by less than 5% sufentanil degradation products by weight, and an MMAD of 0.2 to 3 microns. 50. A condensation aerosol for delivery of nalbuphine, wherein the condensation aerosol is formed by heating a thin layer containing nalbuphine, on a solid support, to produce a vapor of nalbuphine, and condensing the vapor to form a condensation aerosol characterized by less than 5% nalbuphine degradation products by weight, and an MMAD of 0.2 to 3 microns. 51. A condensation aerosol for delivery of fentanyl, wherein the condensation aerosol is formed by heating a thin layer containing fentanyl, on a solid support, to produce a vapor of fentanyl, and condensing the vapor to form a condensation aerosol characterized by less than 5% fentanyl degradation products by weight, and an MMAD of 0.2 to 3 microns. 52. A method of producing naltrexone in an aerosol form comprising: a. heating a thin layer containing naltrexone, on a solid support, to produce a vapor of naltrexone, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% naltrexone degradation products by weight, and an MMAD of 0.2 to 3 microns. 53. A method of producing buprenorphine in an aerosol form comprising: a. heating a thin layer containing buprenorphine, on a solid support, to produce a vapor of buprenorphine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% buprenorphine degradation products by weight, and an MMAD of 0.2 to 3 microns. 54. A method of producing naloxone in an aerosol form comprising: a. heating a thin layer containing naloxone, on a solid support, to produce a vapor of naloxone, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% naloxone degradation products by weight, and an MMAD of 0.2 to 3 microns. 55. A method of producing butorphanol in an aerosol form comprising: a. heating a thin layer containing butorphanol, on a solid support, to produce a vapor of butorphanol, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% butorphanol degradation products by weight, and an MMAD of 0.2 to 3 microns. 56. A method of producing hydromorphone in an aerosol form comprising: a. heating a thin layer containing hydromorphone, on a solid support, to produce a vapor of hydromorphone, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% hydromorphone degradation products by weight, and an MMAD of 0.2 to 3 microns. 57. A method of producing oxycodone in an aerosol form comprising: a. heating a thin layer containing oxycodone, on a solid support, to produce a vapor of oxycodone, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% oxycodone degradation products by weight, and an MMAD of 0.2 to 3 microns. 58. A method of producing methadone in an aerosol form comprising: a. heating a thin layer containing methadone, on a solid support, to produce a vapor of methadone, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% methadone degradation products by weight, and an MMAD of 0.2 to 3 microns. 59. A method of producing remifentanil in an aerosol form comprising: a. heating a thin layer containing remifentanil, on a solid support, to produce a vapor of remifentanil, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% remifentanil degradation products by weight, and an MMAD of 0.2 to 3 microns. 60. A method of producing sufentanil in an aerosol form comprising: a. heating a thin layer containing sufentanil, on a solid support, to produce a vapor of sufentanil, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% sufentanil degradation products by weight, and an MMAD of 0.2 to 3 microns. 61. A method of producing nalbuphine in an aerosol form comprising: a. heating a thin layer containing nalbuphine, on a solid support, to produce a vapor of nalbuphine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% nalbuphine degradation products by weight, and an MMAD of 0.2 to 3 microns. 62. A method of producing fentanyl in an aerosol form comprising: a. heating a thin layer containing fentanyl, on a solid support, to produce a vapor of fentanyl, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% fentanyl degradation products by weight, and an MMAD of 0.2 to 3 microns.
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