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Details for Patent: 6,797,259

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Details for Patent: 6,797,259

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 a muscle relaxant that is used in inhalation therapy. In a composition aspect of the present invention, the aerosol comprises particles comprising at least 5 percent by weight of muscle relaxant. In a method aspect of the present invention, a muscle relaxant is delivered to a mammal through an inhalation route. The method comprises: a) heating a composition, wherein the composition comprises at least 5 percent by weight of a muscle relaxant, to form a vapor; and, b) allowing the vapor to cool, thereby forming a condensation aerosol comprising particles, which is inhaled by the mammal. In a kit aspect of the present invention, a kit for delivering a muscle relaxant through an inhalation route to a mammal is provided which comprises: a) a composition comprising at least 5 percent by weight of a muscle relaxant; and, b) a device that forms a muscle relaxant containing aerosol from the composition, for inhalation by the mammal.
Inventor(s): Rabinowitz; Joshua D. (Mountain View, CA), Zaffaroni; Alejandro C. (Atherton, CA)
Assignee: Alexza Molecular Delivery Corporation (Palo Alto, CA)
Filing Date:May 15, 2002
Application Number:10/150,267
Claims:1. A composition for delivery of a muscle relaxant comprising a condensation aerosol a) formed by volatilizing a muscle relaxant under conditions effective to produce a heated vapor of the muscle relaxant and condensing the heated vapor of the muscle relaxant to form condensation aerosol particles; b) wherein said condensation aerosol particles are characterized by less than 5% muscle relaxant degradation products, and c) the aerosol has an MMAD less than 3 microns.

2. A composition for delivery quinine, chlorzoxazone, carisprodol or cyclobenzaprine comprising a condensation aerosol a) formed by volatilizing quinine, chlorzoxazone, carisprodol or cyclobenzaprine under conditions effective to produce a heated vapor of quinine, chlorzoxazone, carisprodol or cyclobenzaprine comprising and condensing the heated vapor of the quinine, chlorzoxazone, carisprodol or cyclobenzaprine to form condensation aerosol particles; b) wherein said condensation aerosol particles are characterized by less than 5% quinine, chlorzoxazone, carisprodol or cyclobenzaprine degradation products, and c) the aerosol has an MMAD less than 3 microns.

3. The composition according to claim 2, wherein the condensation aerosol particles comprise less than 2.5 percent by weight of quinine, chlorzoxazone, carisprodol or cyclobenzaprine degradation products.

4. The composition according to claim 2, wherein the aerosol particles comprise at least 95 percent by weight of quinine, chlorzoxazone, carisprodol or cyclobenzaprine.

5. The composition according to claim 4, wherein the aerosol has a mass median aerodynamic diameter less than 2 microns.

6. The composition according to claim 6, wherein the aerosol particles comprise at least 97 percent by weight of quinine, chlorzoxazone, carisprodol or cyclobenzaprine.

7. A method of producing quinine, chlorzoxazone, carisprodol or cyclobenzaprine in an aerosol form comprising: a) volatilizing quinine, chlorzoxazone, carisprodol or cyclobenzaprine under conditions effective to produce a heated vapor of the drug, and b) during said volatilizing, passing air through the heated vapor to produce aerosol particles of the quinine, chlorzoxazone, carisprodol or cyclobenzaprine comprising less than 5% quinine, chlorzoxazone, carisprodol or cyclobenzaprine degradation products and an aerosol having an MMAD less than 3 microns.

8. The method according to claim 7, wherein the aerosol particles formed at a rate of greater than 0.5 mg/sec.

9. The method according to claim 7, wherein said volatilizing includes heating a coating, which includes quinine, chlorzoxazone, carisprodol or cyclobenzaprine and is on a solid support having the surface texture of a metal foil, to a temperature sufficient to volatilize quinine, chlorzoxazone, carisprodol or cyclobenzaprine from the coating.

10. The method according to claim 7, wherein the aerosol particles comprise less than 2.5 percent by weight of quinine, chlorzoxazone, carisprodol or cyclobenzaprine degradation products.

11. The method according to claim 9, wherein the aerosol particles comprise at least 95 percent by weight of quinine, chlorzoxazone, carisprodol or cyclobenzaprine.

12. The method according to claim 11, wherein the aerosol has a mass median aerodynamic diameter less than 2 microns.

13. The method according to claim 12, wherein the aerosol particles comprise at least 97 percent by weight of quinine, chlorzoxazone, carisprodol or cyclobenzaprine.

14. A method of producing a muscle relaxant in an aerosol form comprising: a) volatilizing a muscle relaxant under conditions effective to produce a heated vapor of the muscle relaxant, and b) during said volatilizing, passing air through the heated vapor to produce aerosol particles of the muscle relaxant comprising less than 5% muscle relaxant degradation products and an aerosol having an MMAD less than 3 microns.
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