IP Library Granted Patent US 10,413,513
Granted Patent B2
US 10,413,513 · App. 15/885,416 · Granted Sep 17, 2019

Heat-stable dry powder pharmaceutical compositions and methods

Inventors: Karine Fabio (Woodbury, CT); Joseph J. Guarneri (Stamford, CT); Kieran Curley (Cos Cob, CT); Marshall L. Grant (Newtown, CT); Andrea Leone-Bay (Ridgefield, CT)
Assignee: Mannkind Corporation
A61K9/1623A61K9/0073A61K9/1611A61K9/1617A61K31/198A61K31/4172A61K38/095A61K38/12A61K38/23A61K38/26A61K38/28A61K38/29A61K45/06
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Quick Facts
Patent No.
US 10,413,513
App. No.
15/885,416
Granted
Sep 17, 2019
Kind
B2
Abstract

Disclosed herein are heat-stable dry powders which include peptides or protein such as oxytocin for use as a pharmaceutical composition. The composition is highly stable at increased temperatures and relatively high humid environments, and are intended for storage at room temperature with an improved shelf-life. In particular, the dry powders are intended for inhalation, however, other routes of administration can be used when reconstituted in solution.

Claims (23)

1. A method of treating or preventing post-partum hemorrhaging comprising, administering to a subject in need of treatment a dry powder pharmaceutical formulation comprising an oxytocin synthetic peptide, a derivative or analog of said peptide; zinc citrate or zinc chloride, and/or a pharmaceutically acceptable carrier or excipient wherein the formulation is stable for at least 40 weeks at 40° C., 75% relative humidity.

2. The method of claim 1 , wherein the formulation comprises zinc chloride.

3. The method of claim 1 , wherein the pharmaceutically acceptable carrier or excipient is a sugar selected from mannose, mannitol, trehalose, or sorbitol.

4. The method of claim 1 , wherein the pharmaceutically acceptable carrier or excipient is polyvinylpyrrolidone, polyethylene glycol, or a diketopiperazine.

5. The method of claim 4 , wherein the diketopiperazine is fumaryl diketopiperazine or succinyl diketopiperazine.

6. The method of claim 1 , wherein the zinc citrate or zinc chloride is in an amount ranging from 100 to 20 equivalents per mole of the oxytocin, the oxytocin analog or derivative thereof.

7. The method of claim 1 , wherein said oxytocin synthetic peptide, a derivative, or an analog of said peptide is in an amount comprising up to 200 IU.

8. The method of claim 7 , wherein said oxytocin synthetic peptide, a derivative, or an analog of said peptide is in an amount comprising up to 150 IU.

9. The method of claim 7 , wherein said oxytocin synthetic peptide, a derivative, or an analog of said peptide is in an amount comprising up to 100 IU.

10. The method of claim 1 , wherein said oxytocin synthetic peptide, a derivative, or an analog of said peptide is in an amount comprising up to 200 IU.

11. The method of claim 1 , wherein said oxytocin synthetic peptide, a derivative, or an analog of said peptide is in an amount comprising up to 150 IU.

12. The method of claim 1 , wherein said oxytocin synthetic peptide, a derivative, or an analog of said peptide is in an amount comprising up to 100 IU.

13. The method of claim 1 , wherein said oxytocin synthetic peptide, a derivative, or an analog of said peptide is in an amount comprising up to 50 IU, wherein the formulation comprises zinc citrate.

14. The method of claim 1 , further comprising an amino acid selected from leucine, isoleucine, trileucine, cysteine, lysine, glycine, arginine, methionine, and histidine.

15. The method of claim 14 , wherein the amino acid is leucine.

16. The method of claim 14 , wherein the amino acid is isoleucine.

17. The method of claim 14 , wherein the amino acid is trileucine.

18. The method of claim 14 , wherein the amino acid is cysteine.

19. The method of claim 14 , wherein the amino acid is lysine.

20. The method of claim 14 , wherein the amino acid is glycine.

21. The method of claim 14 , wherein the amino acid is arginine.

22. The method of claim 14 , wherein the amino acid is methionine.

23. The method of claim 14 , wherein the amino acid is histidine.

Assignments (5)
PATENT SECURITY AGREEMENT Recorded Aug 12, 2025
From: MANNKIND CORPORATION
To: WILMINGTON TRUST, NATIONAL ASSOCIATION, AS COLLATERAL AGENT
Reel/Frame 072444/0525 →
RELEASE OF SECURITY INTEREST Recorded Apr 5, 2024
From: MIDCAP FINANCIAL TRUST, AS AGENT
To: MANNKIND CORPORATION; MANNKIND LLC
Reel/Frame 067024/0082 →
RELEASE OF SECURITY INTEREST Recorded Aug 13, 2019
From: DEERFIELD PRIVATE DESIGN FUND II, L.P.; DEERFIELD PRIVATE DESIGN INTERNATIONAL II, L.P.; HORIZON SANTE FLML SARL
To: MANNKIND CORPORATION
Reel/Frame 050044/0138 →
SECURITY INTEREST Recorded Aug 13, 2019
From: MANNKIND CORPORATION; MANNKIND LLC
To: MIDCAP FINANCIAL TRUST, AS AGENT
Reel/Frame 050044/0181 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 8, 2018
From: FABIO, KARINE; GUARNERI, JOSEPH J.; CURLEY, KIERAN; GRANT, MARSHALL L.
To: MANNKIND CORPORATION
Reel/Frame 047455/0150 →
Continuity (3)
Continuation 14905236
Provisional Application 61847981 · Jul 18, 2013
Related Publication 20180221280A1 · Aug 9, 2018