Delivery of analgesics through an inhalation route
View Patent ↗The present invention relates to the delivery of analgesics through an inhalation route. Specifically, it relates to aerosols containing acetaminophen, orphenadrine or tramadol that are used in inhalation therapy. In a method aspect of the present invention, an analgesic is administered to a patient through an inhalation route. The method comprises: a) heating a thin layer of acetaminophen, orphenadrine or tramadol, on a solid support to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% acetaminophen, orphenadrine or tramadol degradation products. In a kit aspect of the present invention, a kit for delivering acetaminophen, orphenadrine or tramadol through an inhalation is provided which comprises: a) a thin coating of an acetaminophen, orphenadrine or tramadol composition and b) a device for dispensing said thin coating as a condensation aerosol.
1. A condensation aerosol for delivery of a drug selected from the group consisting of acetaminophen, orphenadrine and tramadol, 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 acetaminophen, orphenadrine and tramadol 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 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 1 , wherein the condensation aerosol is characterized by an MMAD of about 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 acetaminophen.
14. The condensation aerosol according to claim 1 , wherein the drug is orphenadrine.
15. The condensation aerosol according to claim 1 , wherein the drug is tramadol.
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 4 , 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 acetaminophen.
23. The method according to claim 4 , wherein the drug is orphenadrine.
24. The method according to claim 4 , wherein the drug is tramadol.
25. A condensation aerosol for delivery of acetaminophen, wherein the condensation aerosol is formed by heating a thin layer containing acetaminophen, on a solid support, to produce a vapor of acetaminophen, and condensing the vapor to form a condensation aerosol characterized by less than 5% acetaminophen degradation products by weight, and an MMAD of about 0.2 to 3 microns.
26. A condensation aerosol for delivery of orphenadrine, wherein the condensation aerosol is formed by heating a thin layer containing orphenadrine, on a solid support, to produce a vapor of orphenadrine, and condensing the vapor to form a condensation aerosol characterized by less than 5% orphenadrine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
27. A condensation aerosol for delivery of tramadol, wherein the condensation aerosol is formed by heating a thin layer containing tramadol, on a solid support, to produce a vapor of tramadol, and condensing the vapor to form a condensation aerosol characterized by less than 5% tramadol degradation products by weight, and an MMAD of about 0.2 to 3 microns.
28. A method of producing acetaminophen in an aerosol form comprising:
a. heating a thin layer containing acetaminophen, on a solid support, to produce a vapor of acetaminophen, and
b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% acetaminophen degradation products by weight, and an MMAD of about 0.2 to 3 microns.
29. A method of producing orphenadrine in an aerosol form comprising:
a. heating a thin layer containing orphenadrine, on a solid support, to produce a vapor of orphenadrine, and
b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% orphenadrine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
30. A method of producing tramadol in an aerosol form comprising:
a. heating a thin layer containing tramadol, on a solid support, to produce a vapor of tramadol, and
b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% tramadol degradation products by weight, and an MMAD of about 0.2 to 3 microns.