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Last Updated: March 28, 2024

Details for Patent: 6,855,310


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Title: Delivery of analgesics through an inhalation route
Abstract: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 composition aspect of the present invention, the aerosol comprises particles comprising at least 5 percent by weight of acetaminophen, orphenadrine or tramadol. In a method aspect of the present invention, one of acetaminophen, orphenadrine or tramadol 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 acetaminophen, orphenadrine or tramadol, 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 acetaminophen, orphenadrine or tramadol through an inhalation route to a mammal is provided which comprises: a) a composition comprising at least 5 percent by weight of acetaminophen, orphenadrine or tramadol; and, b) a device that forms an acetaminophen, orphenadrine or tramadol 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 16, 2002
Application Number:10/151,596
Claims:1. A composition for delivery of acetaminophen, orphenadrine or tramadol comprising a condensation aerosol a) formed by volatilizing acetaminophen, orphenadrine or tramadol under conditions effective to produce a heated vapor of acetaminophen, orphenadrine or tramadol and condensing the heated vapor of the acetaminophen, orphenadrine or tramadol to form condensation aerosol particles, b) wherein said condensation aerosol particles are characterized by less than 5% acetaminophen, orphenadrine or tramadol degradation products, and c) wherein the aerosol MMAD is less than 3 microns.

2. The composition according to claim 1, wherein the condensation aerosol particles are characterized by less than 2.5 percent by weight of acetaminophen, orphenadrine or tramadol degradation products.

3. The composition according to claim 1, wherein the condensation aerosol particles comprise at least 90 percent by weight of acetaminophen, orphenadrine or tramadol.

4. The composition according to claim 3, wherein the condensation aerosol has a mass median aerodynamic diameter less than 2 microns.

5. The composition according to claim 4, wherein the condensation aerosol particles comprise at least 97 percent by weight of acetaminophen, orphenadrine or tramadol.

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

7. The method according to claim 6, wherein said volatilizing includes heating a thin layer which includes an analgesic selected from the group of acetaminophen, orphenadrine or tramadol and which is on a solid support having the surface texture of a metal foil, to a temperature sufficient to volatilize the analgesic from the thin layer.

8. The method according to claim 7, wherein the aerosol particles comprise less than 2.5 percent by weight of acetaminophen, orphenadrine or tramadol degradation products.

9. The method according to claim 7, wherein the aerosol particles comprise at least 90 percent by weight of acetaminophen, orphenadrine or tramadol.

10. The method according to claim 9, wherein the aerosol has a mass median aerodynamic diameter less than 2 microns.

11. The method according to claim 10, wherein the aerosol particles comprise at least 97 percent by weight of acetaminophen, orphenadrine or tramadol.

12. A composition for delivery of an analgesic comprising a condensation aerosol a) formed by volatilizing an analgesic under conditions effective to produce a heated vapor of the analgesic and condensing the heated vapor of the analgesic to form condensation aerosol particles, b) wherein said condensation aerosol particles are characterized by less than 5% analgesic degradation products, and c) wherein the aerosol MMAD is less than 3 microns.

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