Delivery of caffeine through an inhalation route

• US 7,078,016 B2
• Filed: 11/21/2002
• Issued: 07/18/2006
• Est. Priority Date: 11/21/2001
• Status: Expired due to Fees

• Current Assignee: Alexza Pharmaceuticals Inc. (Grupo Ferrer Internacional SA)
• Original Assignee: Alexza Pharmaceuticals Inc. (Grupo Ferrer Internacional SA)
• Inventors: Rabinowitz, Joshua D.
• Primary Examiner(s): Hartley, Michael G.
• Assistant Examiner(s): Haghighatian, M.
• Application Number:
  US10/302,010
• Publication Number:
  US 20030138382A1
• Time in Patent Office: 1,335 Days
• Field of Search: 424/45, 424/46, 128/200.14, 128/200.24, 604/290, 604/310, 514/264
• US Class Current: 424/45
• CPC Class Codes: A61K 31/52 Purines, e.g. adenine
• CPC Class Codes: A61K 31/522 having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• 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 caffeine through an inhalation route. Specifically, it relates to aerosols containing caffeine 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 caffeine. In a method aspect of the present invention, caffeine 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 caffeine, 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 caffeine through an inhalation route to a mammal is provided which comprises: a) a composition comprising at least 5 percent by weight of caffeine; and, b) a device that forms a caffeine containing aerosol from the composition, for inhalation by the mammal.

Claims

1. A composition for delivery of caffeine, comprising a condensation aerosol,

a) formed by volatilizing caffeine under conditions effective to produce a heated vapor of caffeine and condensing the heated vapor of caffeine to form condensation aerosol particles,

b) wherein the particles are characterized by less than 5% caffeine degradation products, and

c) the aerosol has an MMAD of less than 3 μ

m.

2. The composition according to claim 1, wherein the particles comprise at least 95 percent by weight of caffeine.

3. The composition according to claim 1, wherein the particles comprise at least 97 percent by weight of caffeine.

4. The composition according to claim 3, wherein the particles are characterized by less than 2.5 percent by weight of caffeine degradation products.

5. The composition according to claim 3, wherein the aerosol has an inhalable aerosol drug mass density of between 3 mg/L and 30 mg/l.

6. The composition according to claim 3, wherein the aerosol has an inhalable aerosol particle density of greater than 10⁸ particles/mL.

7. The composition according to claim 3, wherein the aerosol has an MMAD of less than 2.

8. A method of producing caffeine in an aerosol form comprising:

a. volatilizing caffeine under conditions effective to produce a heated vapor of the caffeine and

b. during said volatilizing, passing air through the heated vapor to produce aerosol particles of caffeine comprising less than 5% caffeine degradation products; and

c. an aerosol having an MMAD of less than 3 μ

m.

9. The method according to claim 8, wherein the aerosol particles comprise at least 95 percent by weight of caffeine.

10. The method according to claim 8, wherein the aerosol particles comprise at least 97 percent by weight of caffeine.

11. The method according to claim 10, wherein the aerosol particles comprise less than 1 percent by weight of caffeine degradation products.

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

13. The method according to claim 8, wherein said volatilizing includes heating caffeine on a solid support having the surface texture of a metal foil, to a temperature sufficient to volatilize the caffeine.

14. The method according to claim 8, wherein the aerosol particles comprise less than 2.5 percent by weight of caffeine degradation products.