Delivery of caffeine through an inhalation route

• US 20060257328A1
• Filed: 07/18/2006
• Published: 11/16/2006
• Est. Priority Date: 11/21/2001
• 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.
• Granted Patent: US 7,488,469 B2
• Time in Patent Office: Days
• US Class Current: 424/46
• 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. An aerosol comprising particles, wherein the particles comprise at least 5 percent by weight of caffeine.

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

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

4. The aerosol according to claim 3, wherein the aerosol comprises less than 1 percent by weight of caffeine degradation products.

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

7. The aerosol according to claim 3, wherein the particles have a mass median aerodynamic diameter less than 2.

8. The aerosol according to claim 3, wherein the aerosol is formed by heating a composition containing caffeine to form a vapor, which subsequently condenses to form an aerosol.

9. A method for delivering caffeine to a mammal through an inhalation route, wherein 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.

10. The method according to claim 9, wherein the aerosol comprises at least 95 percent by weight of caffeine.

11. The method according to claim 9, wherein the aerosol comprises at least 97 percent by weight of caffeine.

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

13. A kit for delivering caffeine through an inhalation route to a mammal, wherein the kit 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.

14. The kit according to claim 13, wherein the composition comprises at least 90 percent by weight of caffeine.

15. The kit according to claim 14, wherein the device contained in the kit comprises:

a) an element for heating the caffeine composition to form a vapor;

b) an element allowing the vapor to cool to form an aerosol; and

,

c) an element permitting the mammal to inhale the aerosol.