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Details for Patent: 7,108,847

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Details for Patent: 7,108,847

Title:Delivery of muscle relaxants through an inhalation route
Abstract: 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.
Inventor(s): Rabinowitz; Joshua D. (Mountain View, CA), Zaffaroni; Alejandro C. (Atherton, CA)
Assignee: Alexza Pharmaceuticals, Inc. (Palo Alto, CA)
Filing Date:Mar 31, 2004
Application Number:10/814,998
Claims:1. A condensation aerosol for delivery of a drug selected from the group consisting of quinine, chlorzoxazone, carisprodol and cyclobenzaprine, 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.sup.9 particles per second.

3. The condensation aerosol according to claim 2, wherein the condensation aerosol is formed at a rate greater than 10.sup.10 particles per second.

4. A method of producing a drug selected from the group consisting of quinine, chlorzoxazone, carisprodol and cyclobenzaprine 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 of greater than 10.sup.9 particles per second.

6. The method according to claim 5, wherein the condensation aerosol is formed at a rate of greater than 10.sup.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 quinine.

14. The condensation aerosol according to claim 1, wherein the drug is chlorzoxazone.

15. The condensation aerosol according to claim 1, wherein the drug is carisprodol.

16. The condensation aerosol according to claim 1, wherein the drug is cyclobenzaprine.

17. The method according to claim 4, wherein the condensation aerosol is characterized by an MMAD of 0.1 to 5 microns.

18. The method according to claim 4, wherein the condensation aerosol is characterized by an MMAD of less than 3 microns.

19. The method according to claim 4, wherein the condensation aerosol is characterized by an MMAD of about 0.2 to 3 microns.

20. The method according to claim 4, wherein the condensation aerosol is characterized by less than 5% drug degradation products by weight.

21. The method according to claim 20, wherein the condensation aerosol is characterized by less than 2.5% drug degradation products by weight.

22. The method according to claim 4, wherein the solid support is a metal foil.

23. The method according to claim 4, wherein the drug is quinine.

24. The method according to claim 4, wherein the drug is chlorzoxazone.

25. The method according to claim 4, wherein the drug is carisiprodol.

26. The method according to claim 4, wherein the drug is cyclobenzaprine.

27. A condensation aerosol for delivery of quinine, wherein the condensation aerosol is formed by heating a thin layer containing quinine, on a solid support, to produce a vapor of quinine, and condensing the vapor to form a condensation aerosol characterized by less than 5% quinine degradation products by weight, and an MMAD of about 0.2 to 3 microns.

28. A condensation aerosol for delivery of chlorzoxazone, wherein the condensation aerosol is formed by heating a thin layer containing chlorzoxazone, on a solid support, to produce a vapor of chlorzoxazone, and condensing the vapor to form a condensation aerosol characterized by less than 5% chlorzoxazone degradation products by weight, and an MMAD of 0.2 to 3 microns.

29. A condensation aerosol for delivery of carisiprodol, wherein the condensation aerosol is formed by heating a thin layer containing carisiprodol, on a solid support, to produce a vapor of carisiprodol, and condensing the vapor to form a condensation aerosol characterized by less than 5% carisiprodol degradation products by weight, and an MMAD of 0.2 to 3 microns.

30. A condensation aerosol for delivery of cyclobenzaprine, wherein the condensation aerosol is formed by heating a thin layer containing cyclobenzaprine, on a solid support, to produce a vapor of cyclobenzaprine, and condensing the vapor to form a condensation aerosol characterized by less than 5% cyclobenzaprine degradation products by weight, and an MMAD of 0.2 to 3 microns.

31. A method of producing quinine in an aerosol form comprising: a. heating a thin layer containing quinine, on a solid support, to produce a vapor of quinine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% quinine degradation products by weight, and an MMAD of 0.2 to 3microns.

32. A method of producing chlorzoxazone in an aerosol form comprising: a. heating a thin layer containing chlorzoxazone, on a solid support, to produce a vapor of chlorzoxazone, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% chlorzoxazone degradation products by weight, and an MMAD of 0.2 to 3 microns.

33. A method of producing carisiprodol in an aerosol form comprising: a. heating a thin layer containing carisiprodol, on a solid support, to produce a vapor of carisiprodol, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% carisiprodol degradation products by weight, and an MMAD of 0.2 to 3 microns.

34. A method of producing cyclobenzaprine in an aerosol form comprising: a. heating a thin layer containing cyclobenzaprine, on a solid support, to produce a vapor of cyclobenzaprine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% cyclobenzaprine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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