Granted Patent B2

US 8,734,845 · App. 13/377,682 · Granted May 27, 2014

Abstract

Claims (20)

1. Diketopiperazine microparticles having a specific surface area of from about 35 m 2 /g to about 67 m 2 /g.

2. The diketopiperazine microparticles according to claim 1 , wherein said microparticles comprise a drug or active agent.

3. The diketopiperazine microparticles according to claim 2 , wherein said specific surface area is less than about 62 m 2 /g.

4. The diketopiperazine microparticles according to claim 3 , wherein said drug or active agent is a peptide or protein.

5. The diketopiperazine microparticles according to claim 4 , wherein said peptide is an endocrine hormone.

6. The diketopiperazine microparticles according to claim 5 , wherein said endocrine hormone is insulin, parathyroid hormone, calcitonin, glucagon, glucagon-like peptide 1, oxyntomodulin, an analog or active fragment of said endocrine hormone.

7. The diketopiperazine microparticles according to claim 1 , wherein said diketopiperazine is fumaryl diketopiperazine.

8. The diketopiperazine microparticles of claim 6 in a dry powder form.

9. The diketopiperazine microparticles of claim 6 wherein said endocrine hormone is insulin or an analog or active fragment thereof.

10. The diketopiperazine microparticles of claim 6 wherein said endocrine hormone is glucagon-like peptide 1 or an analog or active fragment thereof.

11. The diketopiperazine microparticles of claim 1 having a specific surface area of from about 45 m 2 /g to about 67 m 2 /g.

12. The diketopiperazine microparticles of claim 1 having a specific surface area of from about 35 m 2 /g to about 56 m 2 /g.

13. The diketopiperazine microparticles of claim 1 having a specific surface area of from about 45 m 2 /g to about 56 m 2 /g.

14. The diketopiperazine microparticles of claim 9 wherein said endocrine hormone is insulin.

15. The diketopiperazine microparticles of claim 14 wherein the microparticles are about 10-15% insulin by weight.

16. The diketopiperazine microparticles of claim 5 , wherein said endocrine hormone is an exendin.

17. The diketopiperazine microparticles of claim 14 wherein the microparticles comprise 3-4 U/mg insulin.

18. The diketopiperazine microparticles of claim 15 wherein the microparticles are about 11% insulin.

19. The diketopiperazine microparticles of claim 2 wherein said drug or active agent comprises about 0.01% to about 20% of the weight of the microparticles.

20. A dry powder comprising the diketopiperazine microparticles of claim 19 .

Assignments (8)