PARTICLES FOR INHALATION HAVING RAPID RELEASE PROPERTIES

• US 20080226730A1
• Filed: 09/24/2007
• Published: 09/18/2008
• Est. Priority Date: 12/29/2000
• Status: Abandoned Application

• Current Assignee: Civitas Therapeutics, Inc. (Acorda Therapeutics Incorporated)
• Original Assignee: Civitas Therapeutics, Inc. (Acorda Therapeutics Incorporated)
• Inventors: Edwards, David A., Chen, Donghao, Hrkach, Jeffrey S., Batycky, Richard P., Schmitke, Jennifer L.
• Application Number:
  US11/860,302
• Publication Number:
  US 20080226730A1
• Time in Patent Office: Days
• US Class Current: 424/489
• CPC Class Codes: A61K 38/28 Insulins
• CPC Class Codes: A61K 47/544 Phospholipids
• CPC Class Codes: A61K 9/0075 for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
• CPC Class Codes: A61K 9/1617 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The invention generally relates to formulations having particles comprising phospholipids, bioactive agent and excipients and the pulmonary delivery thereof. Dry powder inhaled insulin formulations are disclosed. Improved formulations comprising DPPC, insulin and sodium citrate which are useful in the treatment of diabetes are disclosed. Also, the invention relates to a method of for the pulmonary delivery of a bioactive agent comprising administering to the respiratory tract of a patient in need of treatment, or diagnosis an effective amount of particles comprising a bioactive agent or any combination thereof in association, wherein release of the agent from the administered particles occurs in a rapid fashion.

Claims

1. A formulation having particles comprising, by weight, 75% DPPC, 15% insulin and 10% sodium citrate.

2. The formulation of claim 1, wherein the particles comprise a mass of from about 1.5 mg to about 20 mg of insulin.

3. The formulation of claim 1, wherein the particles are placed in a receptacle and comprise a mass of about 1.5 mg of insulin per receptacle.

4. The formulation of claim 1, wherein the particles are placed in a receptacle and comprise a mass of about 5 mg of insulin per receptacle.

5. The formulation of claim 1, wherein the particles comprise a dosage of insulin between about 42 IU and about 540 IU.

6. The formulation of claim 5, wherein the particles comprise a dosage of insulin of about 42 IU.

7. The formulation of claim 5, wherein the particles comprise a dosage of insulin of between about 84 IU and about 294 IU.

8. The formulation of claim 1, wherein the particles have a tap density less than about 0.4 g/cm³.

9. The formulation of claim 8, wherein the particles have a tap density less than about 0.1 g/cm³.

10. The formulation of claim 1, wherein the particles have a median geometric diameter of from about 5 micrometers to about 30 micrometers.

11. The formulation of claim 10, wherein the particles have a median geometric diameter of from about 7 micrometers to about 8 micrometers.

12. The formulation of claim 1, wherein the particles have an aerodynamic diameter of from about 1 micrometer to about 5 micrometers.

13. The formulation of claim 12, wherein the particles have an aerodynamic diameter of from about 1 micrometer to about 3 micrometers.

14. A method for treating a human patient in need of insulin comprising administering pulmonarily to the respiratory tract of a patient in need of treatment, an effective amount of particles comprising by weight, 75% DPPC, 15% insulin and 10% sodium citrate, wherein release of the insulin is rapid.

15. The method of claim 14, wherein the particles comprise a dosage of insulin of between about 84 IU and about 294 IU.

16. The method of claim 14 wherein the particles have a tap density less than about 0.4 g/cm³.

17. The method of claim 16, wherein the particles have a tap density less than about 0.1 g/cm³.

18. The method of claim 14, wherein the particles have a median geometric diameter of from about 5 micrometers to about 30 micrometers.

19. A method of delivering an effective amount of insulin to the pulmonary system, comprising:

a) providing a mass of particles comprising by weight, 75% DPPC, 15% insulin and 10% sodium citrate; and

b) administering via simultaneous dispersion and inhalation the particles, from a receptacle having the mass of the particles, to a human subject'"'"'s respiratory tract, wherein release of the insulin is rapid.

20. The method of claim 19, wherein the particles comprise a dosage of insulin of between about 84 IU and about 294 IU.

21. The method of claim 19, wherein the particles have a tap density less than about 0.4 g/cm³.

22. The method of claim 21, wherein the particles have a tap density less than about 0.1 g/cm³.

23. The method of claim 19, wherein the particles have a median geometric diameter of from about 5 micrometers to about 30 micrometers.

24. A kit for administration of insulin comprising two or more receptacles, wherein said receptacles comprise unit dosages of particles comprising, by weight, 75% DPPC, 15% insulin and 10% sodium citrate.

25. The kit of claim 24, wherein said kit further comprises instructions for use of said two or more receptacles.