Generated: May 26, 2017
|Title:||Delivery of diphenhydramine through an inhalation route|
|Abstract:||The present invention relates to the delivery of antihistamines through an inhalation route. Specifically, it relates to aerosols containing diphenhydramine 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 diphenhydramine. In a method aspect of the present invention, diphenhydramine 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 diphenhydramine, 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 diphenhydramine through an inhalation route to a mammal is provided which comprises: a) a composition comprising at least 5 percent by weight of diphenhydramine; and, b) a device that forms a diphenhydramine 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 21, 2002|
|Claims:||1. A composition for delivery of diphenhydramine comprising a condensation aerosol a) formed by volatizing the diphenhydramine under conditions effective to produce a heated vapor of the diphenhydramine and condensing the heated vapor of the diphenhydramine to form condensation aerosol particles, b) wherein said condensation aerosol particles are characterized by less than 5% diphenhydramine degradation products, and c) wherein the aerosol MMAD is less than 3 microns. |
2. The composition according to claim 1, wherein the diphenhydramine is a free base form of diphenhydramine.
3. The composition according to claim 1, wherein the diphenhydramine degradation product is benzophenone.
4. The composition according to claim 1, wherein the condensation aerosel particles comprise at least 90 percent by weight of diphenhydramine.
5. A method of producing diphenhydramine in an aerosol form comprising a) volatilizing diphenhydramine under conditions effective to produce a heated vapor of the diphenhydramine, and b) during said volatilizing, passing air through the heated vapor to produce aerosol particles of the diphenhydramine comprising less than 5% diphenhydramine degradation products and an aerosol having an MMAD less than 3 .mu.m.
6. The method according to claim 5, wherein said volatilizing includes heating a thin layer which includes the diphenhydramine and which is on a solid support having the surface texture of a metal foil, to a temperature sufficient to volatilize the diphenhydramine from the thin layer.
7. The method according to claim 5, wherein the aerosol particles are formed at a rate of greater than 0.5 mg/sec.
8. The method according to claim 5, wherein the diphenhydramine degradation product is benzophenone.
9. The method according to claim 8, wherein the aerosol particles comprise at least 90 percent by weight of diphenhydramine.
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