Details for Patent: 6,716,416

Title:	Delivery of antipsychotics through an inhalation route
Abstract:	The present invention relates to the delivery of antipsychotics through an inhalation route. Specifically, it relates to aerosols containing antipsychotics 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 an antipsychotic. In a method aspect of the present invention, an antipsychotic 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 an antipsychotic, 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 an antipsychotic through an inhalation route to a mammal is provided which comprises: a) a composition comprising at least 5 percent by weight of an antipsychotic; and, b) a device that forms an antipsychotic 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 20, 2002
Application Number:	10/152,639
Claims:	1. A composition for delivery of an antpsychotic compound comprising a condensation aerosol a) formed by volatilizing an antipsychotic compound under conditions effective to produce a heated vapor of the compound, and condensing the heated vapor of the compound to form condensation aerosol particles, and b) wherein said particles are characterized by less than 5% compound degradation products, and c) aerosol MMAD is less than 3 microns. 2. A composition for delivery of an antipsychotic compound comprising a condensation aerosol a) formed by volatilizing an antipsychotic compound selected from the group consisting of olanzapine, trifluoperazine, haloperidol, loxapine, risperidone, clozapine, quetiapine, promazine, thiothixene, chlorpromazine, droperidol, prochlorperazine, or fluphenazine under conditions effective to produce a heated vapor of the compound, and condensing the heated vapor of the compound to form condensation aerosol particles, and b) wherein said condensation aerosol particles are characterized by less than 5% compound degradation products, and c) aerosol MMAD is less than 3 microns. 3. The composition according to claim 2, wherein the condensation aerosol particles are characterized by less than 2.5 percent by weight of olanzapine, trifluoperazine, haloperidol, loxapine, clozapine, quetiapine, promazine, or chlorpromazine degradation products. 4. The composition according to claim 2, wherein the condensation aerosol particles comprise at least 90 percent by weight of olanzapine, trifluoperazine, haloperidol, loxapine, clozapine, quetiapine, promazine, chlorpromazine, prochlorperazine, or fluphenazine. 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 5, wherein the condensation aerosol particles comprise at least 97 percent by weight of olanzapine, trifluoperazine, haloperidol, loxapine, clozapine, quetiapine, promazine, chlorpromazine, or prochlorperazine. 7. A method of producing the antipsychotic compound olanzapine, trifluoperazine, haloperidol, loxapine, risperidone, clozapine, quetiapine, promazine, thiothixene, chlorpromazine, droperidol or fluphenazine in an aerosol form comprising: a) volatilizing an antipsychotic compound selected from the group consisting of olanzapine, trifluoperazine, haloperidol, loxapine, risperidone, clozapine, quetiapine, promazine, thiothixene, chlorpromazine, droperidol or fluphenazine, under conditions effective to produce a heated vapor of the compound, and b) during said volatilizing, passing air through the heated vapor to produce aerosol particles of the compound comprising less than 5% compound degradation products and c) aerosol MMAD is less than 3 microns. 8. The method according to claim 7, wherein the aerosol particles are 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 the antipsychotic compound, and which is formed on a solid support having the surface texture of a metal foil, to a temperature sufficient to volatilize the compound from the coating. 10. The method according to claim 7, wherein the particles comprise less than 2.5 percent by weight of olanzapine, trifluoperazine, haloporidol, loxapine, clozapine, quetiapine, promazine, or chlorpromazine degradation products. 11. The method according to claim 9, wherein the particles comprise at least 90 percent by weight of olanzapine, trifluoperazine, haloperidol, loxapine, clozapine, quetiapine, promazine, chlorpromazine, prochlorperazine, or fluphenazine. 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 particles comprise at least 97 percent by weight of olanzapine, trifluoperazine, haloperidol, loxapine, clozapine, quetiapine, promazine, chlorpromazine, or prochlorperazine.