Delivery of caffeine through an inhalation route

• US 7,488,469 B2
• Filed: 07/18/2006
• Issued: 02/10/2009
• 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): Haghighatian; Mina
• Application Number:
  US11/488,302
• Publication Number:
  US 20060257328A1
• Time in Patent Office: 938 Days
• Field of Search: 424/45, 424/46, 424/434, 424/489, 424/499, 514/958, 218/200.14, 218/200.24, 218/203.15
• 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 condensation aerosol for delivery of caffeine formed by heating a composition containing caffeine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of caffeine and less than 5 percent by weight of caffeine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

2. The condensation aerosol according to claim 1, wherein the condensation aerosol has an MMAD of less than 3 microns.

3. The condensation aerosol according to claim 1 or claim 2, wherein the condensation aerosol has an MMAD of less than 2 microns.

11. The condensation aerosol according to claim 2, wherein the condensing comprises allowing the vapor to cool.

4. A method of forming a caffeine containing aerosol comprising:

(a) heating a composition containing caffeine coated on a solid support to form a vapor; and

(b) condensing the vapor to form a condensation aerosol comprising particles,

wherein the particles comprise less than 5 percent by weight of caffeine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.

5. The method according to claim 4, wherein the condensation aerosol has an MMAD of less than 3 microns.

6. The method according to claim 5, wherein the coated composition comprises at least 10 percent by weight of caffeine.

12. The method according to claim 5, wherein the condensing comprises allowing the vapor to cool.

7. A method of forming a caffeine containing aerosol comprising:

(a) heating a composition containing caffeine and a pharmaceutically acceptable excipient coated on a solid support to form a vapor; and

(b) condensing the vapor to form a condensation aerosol comprising particles,

wherein the particles comprise at least 10 percent by weight of caffeine and less than 5 percent by weight of caffeine degradation products and the condensation aerosol has an MMAD of less than 5 microns.

8. The method according to claim 7, wherein the condensation aerosol has an MMAD of less than 3 microns.

9. The method according to claim 8, wherein the coated composition comprises at least 10 percent by weight of caffeine.

10. The method according to claim 8, wherein the condensing comprises allowing the vapor to cool.

13. A method of forming a caffeine containing aerosol comprising:

(a) heating a composition containing caffeine coated on a solid support to form a vapor, and

(b) condensing the vapor to form a condensation aerosol comprising particles, wherein the condensation aerosol is formed at a rate greater than 1 mg/second, and

wherein the particles comprise at least 10 percent by weight of caffeine and less than 5 percent by weight of caffeine degradation products, and the condensation aerosol has an MMAD less than 5 microns.

14. The method according to claim 13, wherein the condensation aerosol has an MMAD of less than 3 microns.

15. The method according to claim 14, wherein the condensation aerosol is formed at a rate greater than 5 mg/second.

16. The method according to claim 15, wherein the condensation aerosol is formed at a rate greater than 20 mg/second.

17. The method according to claim 13, wherein the condensing comprises allowing the vapor to cool.