Delivery of aerosols containing small particles through an inhalation route

• US 6,682,716 B2
• Filed: 05/13/2002
• Issued: 01/27/2004
• Est. Priority Date: 06/05/2001
• Status: Expired due to Fees

• Current Assignee: Alexza Pharmaceuticals Inc. (Grupo Ferrer Internacional SA)
• Original Assignee: Alexza Molecular Delivery Corporation (Grupo Ferrer Internacional SA)
• Inventors: Lloyd, Peter M., Hodges, Craig C., Wensley, Martin J., Mufson, Daniel, Rogers, Daniel D.
• Primary Examiner(s): Hartley, Michael G.
• Assistant Examiner(s): HAGHIGHATIAN, MINA
• Application Number:
  US10/146,515
• Publication Number:
  US 20030035776A1
• Time in Patent Office: 624 Days
• Field of Search: 424/45, 424/450, 424/46, 424/789, 128/200.14, 128/203.15, 514/54, 514/220, 514/252
• US Class Current: 424/45
• CPC Class Codes: A61K 31/235 having an aromatic ring attached to a carboxyl group
• CPC Class Codes: A61K 31/4468 having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• 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
• CPC Class Codes: A61M 11/001 Particle size control
• CPC Class Codes: A61M 11/02 operated by air or other gas pressure applied to the liquid or other product to be sprayed or atomised sprayers for horticulture A01G, A01H; killing insects A01M; air humidifying by nozzles F24F6/14, F24F6/18; cooling by spraying F28B, F28C
• CPC Class Codes: A61M 11/044 with electrodes immersed in the liquid
• CPC Class Codes: A61M 15/00 Inhalators drug delivery in endotracheal tubes A61M16/04
• CPC Class Codes: A61M 15/0028 using prepacked dosages, one for each application, e.g. capsules to be perforated or broken-up
• CPC Class Codes: A61M 16/109 the humidifying liquid or the beneficial agent
• CPC Class Codes: A61M 2016/0039 in the inspiratory circuit
• CPC Class Codes: A61M 2205/3606 cooled
• CPC Class Codes: A61M 2205/3653 by Joule effect, i.e. electric resistance
• CPC Class Codes: A61M 2205/368 by electromagnetic radiation, e.g. IR waves
• CPC Class Codes: A61M 2205/50 with microprocessors or computers
• CPC Class Codes: A61P 23/00 Anaesthetics
• CPC Class Codes: B05B 17/04 operating with special methods
• CPC Class Codes: B05B 7/1686 involving vaporisation of the material to be sprayed or of an atomising-fluid-generating product

Abstract

The present invention relates to the inhalation delivery of aerosols containing small particles. Specifically, it relates to the delivery of drug containing aerosols having particles with a mass median aerodynamic diameter less than 1μ for inhalation therapy. In a composition aspect of the present invention the drug containing aerosol comprises particles having a mass median aerodynamic diameter between 10 nm and 1μ. Preferably, the particles have a mass median aerodynamic diameter between 10 nm and 900 nm. More preferably, the particles have a mass median aerodynamic diameter between 10 nm and 800 nm, 10 nm and 700 nm, 10 nm and 600 nm, 10 nm and 500 nm, 10 nm and 400 nm, 10 nm and 300 nm, 10 nm and 200 nm, or 10 nm and 100 nm.

Claims

1. A composition for inhalation therapy, comprising an aerosol of vaporized drug condensed into particles, wherein said aerosol has a mass median aerodynamic diameter between 10 nm and 100 nm.

2. The composition according to claim 1, wherein the mass of the aerosol is at least 0.05 mg.

3. The composition according to claim 2, wherein the particles comprise at least 5 percent by weight of drug.

4. The composition according to claim 3, wherein the particles comprise less than 10 percent by weight of drug degradation products.

5. The composition according to claim 4, wherein the aerosol has a geometric standard deviation around the mass median aerodynamic diameter of less than 2.

6. The composition according to claim 5, wherein the drug is an antibiotic.

7. The composition according to claim 5, wherein the drug is an anticonvulsant.

8. The composition according to claim 5, wherein the drug is an antidepressant.

9. The composition according to claim 5, wherein the drug is an antiemetic.

10. The composition according to claim 5, wherein the drug is an antihistamine.

11. The composition according to claim 5, wherein the drug is an antiparkinsonian drug.

12. The composition according to claim 5, wherein the drug is an anxiolytic.

13. The composition according to claim 5, wherein the drug is a drug for erectile dysfunction.

14. The composition according to claim 5, wherein the drug is a drug for migraine headaches.

15. The composition according to claim 5, wherein the drug is a drug for the treatment of alcoholism.

16. The composition according to claim 5, wherein the drug is a drug for the treatment of addiction.

17. The composition according to claim 5, wherein the drug is a muscle relaxant.

18. The composition according to claim 5, wherein the drug is a non-steroidal anti-inflammatory.

19. The composition according to claim 5, wherein the drug is an opioid.

20. The composition according to claim 5, wherein the drug is an other analgesic.

21. The composition according to claim 5, wherein the drug is a stimulant.

22. The composition of claim 1 wherein the drug particles comprise at least 40 percent by weight of a drug.

23. The composition of claim 1 wherein the drug particles comprise at least 50 percent by weight of a drug.

24. A composition for inhalation therapy, comprising a condensation aerosol of drug, wherein the aerosol has a mass median aerodynamic diameter between 10 nm and 100 nm and the drug is characterized by a decomposition index of less than 0.15.

25. A composition for inhalation therapy, comprising an aerosol of condensation drug particles, wherein the aerosol has a mass median aerodynamic diameter between 10 nm and 100 nm, and is essentially devoid of solvents.