Delivery of diazepam through an inhalation route

• US 20060269486A1
• Filed: 08/07/2006
• Published: 11/30/2006
• Est. Priority Date: 11/09/2001
• Status: Active Grant

• Current Assignee: Alexza Pharmaceuticals Inc. (Grupo Ferrer Internacional SA)
• Original Assignee: Alexza Pharmaceuticals Inc. (Grupo Ferrer Internacional SA)
• Inventors: Rabinowitz, Joshua D., Zaffaroni, Alejandro C.
• Granted Patent: US 7,470,421 B2
• Time in Patent Office: Days
• US Class Current: 424/46
• CPC Class Codes: A61K 31/5513 1,4-Benzodiazepines, e.g. diazepam or clozapine
• CPC Class Codes: A61K 9/007 Pulmonary tract; Aromatherapy
• CPC Class Codes: A61K 9/0073 Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy; nasal sprays A61K9/0043; inhalation of vapours of volatile or heated drugs, e.g. essential oils or nicotine, A61K9/007; devices A61M

Abstract

The present invention relates to the delivery of compounds for the treatment of anxiety disorders and symptoms of such disorders through an inhalation route. Specifically, it relates to aerosols containing diazepam that are used in inhalation therapy. In a method aspect of the present invention, diazepam is administered to a patient through an inhalation route. The method comprises: a) heating a thin layer of diazepam on a solid support to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% drug degradation products. In a kit aspect of the present invention, a kit for delivering diazepam through an inhalation route is provided which comprises: a) a thin coating of a diazepam composition; and, b) a device for dispending said thin coating as a condensation aerosol.

Claims

1. A composition for delivery of diazepam consisting of a condensation aerosol

a) formed by volatilizing a thin layer of diazepam on a solid support, having the surface texture of a metal foil, to a temperature sufficient to produce a heated vapor of diazepam and condensing the heated vapor of diazepam to form condensation aerosol particles,

b) wherein said condensation aerosol particles are characterized by less than 5% diazepam degradation products, and

c) the condensation aerosol has an MMAD of less than 3 microns.

2. The composition according to claim 1, wherein the aerosol particles are formed at a rate of at least 10⁹ particles per second.

3. The composition according to claim 2, wherein the aerosol particles are formed at a rate of at least 10¹⁰ particles per second.

4. The composition according to claim 1, wherein said condensation aerosol particles are characterized by less than 2.5% diazepam degradation products.

5. A method of producing diazepam in an aerosol form comprising:

a. heating a thin layer of diazepam on a solid support, having the surface texture of a metal foil, to a temperature sufficient to volatilize the diazepam to form a heated vapor of the diazepam, and

b. during said heating, passing air through the heated vapor to produce aerosol particles of the diazepam comprising less than 5% diazepam degradation products, and an aerosol having an MMAD of less than 3 microns.

6. The method according to claim 5, wherein the aerosol particles are formed at a rate of greater than 10⁹ particles per second.

7. The method according to claim 6, wherein the aerosol particles are formed at a rate of greater than 10¹⁰ particles per second.

8. The composition according to claim 5, wherein said aerosol particles are comprise less than 2.5% diazepam degradation products.