IP Library Granted Patent US 9,737,518
Granted Patent B2
US 9,737,518 · App. 14/870,736 · Granted Aug 22, 2017

Tiotropium dry powders

Inventors: Jean C. Sung (Cambridge, MA); Diana Manzanedo (Cambridge, MA); Jason M. Perry (Cambridge, MA); Wesley Dehaan (Chelmsford, MA); Brian Trautman (Arlington, MA)
Assignee: Pulmatrix Operating Company, Inc.
A61K31/439A61K9/0075A61K9/1611A61K9/1617A61K31/57A61K31/58A61K45/06
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Quick Facts
Patent No.
US 9,737,518
App. No.
14/870,736
Granted
Aug 22, 2017
Kind
B2
Abstract

The present invention relates to respirable dry powder comprising respirable dry particles that comprise sodium chloride, leucine, and tiotropium bromide, wherein the sodium chloride is about 60% to about 90%, the leucine is about 10% to about 40%, the tiotropium bromide is about 0.01% to about 0.5%, and optionally one or more additional therapeutic agents up to about 20%, wherein all percentages are weight percentages on a dry basis and all the components of the respirable dry particles amount to 100%. The invention also relates to respirable dry powders that contain respirable dry particles that comprise sodium chloride, leucine, and tiotropium bromide, wherein the sodium chloride is 67% to 84%, the leucine is 12% to 28%, the tiotropium bromide is about 0.01% to about 0.5%, and optionally one or more additional therapeutic agents up to about 20%, wherein all percentages are weight percentages on a dry basis and all the components of the respirable dry particles amount to 100%. The invention also relates to respirable dry powders that contain respirable dry particles that comprise about 79.5% to about 80.5% (w/w) sodium chloride, about 19.5% to about 20.5% (w/w) leucine, and about 0.01% to about 0.5% (w/w) tiotropium bromide, and methods for treating a subject using the respirable dry powders.

Claims (23)

1. A receptacle comprising a respirable dry powder consisting of homogenous respirable dry particles that comprise sodium chloride, leucine, and tiotropium bromide, wherein the sodium chloride is 67% to 84% by weight, the leucine is 12% to 28% by weight, the tiotropium bromide is about 0.01% to about 0.5% by weight, and optionally one or more additional therapeutic agents up to about 20% by weight, wherein all percentages are weight percentages on a dry basis and all the components of the respirable dry particles amount to 100%, wherein the receptacle contains a nominal dose of tiotropium between about 1.5 to about 12 micrograms.

2. The receptacle of claim 1 , wherein the receptacle is a capsule or a blister, and wherein the receptacle contains about 15 mg of dry powder or less.

3. The receptacle of claim 1 , wherein the receptacle contains a nominal dose of tiotropium between about 3 to about 12 micrograms.

4. The receptacle of claim 1 , wherein the receptacle contains a nominal dose of tiotropium between about 3 to about 9 micrograms.

5. The receptacle of claim 1 , wherein the receptacle contains a nominal dose of tiotropium between about 3 to about 6 micrograms.

6. The receptacle of claim 1 , wherein the respirable dry powder has a fine particle dose less than 5.0 microns of between about 1 microgram and about 5 micrograms of tiotropium.

7. The receptacle of claim 1 , wherein the respirable dry powder has a fine particle dose less than 4.4 microns of between about 1 microgram and about 4 micrograms of tiotropium.

8. The receptacle of claim 1 , wherein the respirable dry powder has a fine particle dose less than 4.4 microns of between about 1.5 micrograms and about 3.5 micrograms of tiotropium.

9. The receptacle of claim 1 , wherein the receptacle is a capsule, and wherein the capsule contains less than 6 mg of dry powder.

10. The receptacle of claim 1 , wherein the sodium chloride is about 79.5% to about 80.5% by weight and the leucine is about 19.5% to about 20.5% by weight.

11. The receptacle of claim 1 , wherein the respirable dry particles have a volume median geometric diameter (VMGD) of about 5 micrometers or less.

12. The receptacle of claim 1 , wherein the respirable dry powder has a mass median aerodynamic diameter (MMAD) of between about 1 micron and about 5 microns.

13. The receptacle of claim 1 , wherein the respirable dry particles have a 1/4 bar dispersibility ratio (1/4 bar) of less than 1.5 as measured by laser diffraction.

14. The receptacle of claim 1 , wherein the respirable dry particles have a tap density greater than 0.4 g/cc to about 1.2 g/cm 3 .

15. The receptacle of claim 1 , wherein the one or more additional therapeutic agent is one or more corticosteroids.

16. A receptacle comprising a respirable dry powder consisting of homogenous respirable dry particles that comprise sodium chloride, leucine, and tiotropium bromide, wherein the sodium chloride is 67% to 84% by weight, the leucine is 12% to 28% by weight, the tiotropium bromide is about 0.01% to about 0.5% by weight, and optionally one or more additional therapeutic agents up to about 20% by weight, wherein all percentages are weight percentages on a dry basis and all the components of the respirable dry particles amount to 100%, wherein the receptacle contains a nominal dose of tiotropium between about 0.5 to about 6 micrograms.

17. The receptacle of claim 16 , wherein the receptacle contains a nominal dose of tiotropium between about 0.5 microgram to about 3 micrograms.

18. The receptacle of claim 16 , wherein the respirable dry powder has a fine particle dose less than 5.0 microns of between about 1 microgram and about 5 micrograms of tiotropium.

19. The receptacle of claim 1 , wherein the respirable dry powder has a fine particle dose less than 4.4 microns of between about 1.5 micrograms and about 3.5 micrograms of tiotropium.

20. A method for treating a respiratory disease selected from the group consisting of COPD, chronic bronchitis, emphysema, asthma, cystic fibrosis, or non-cystic fibrosis bronchiectasis, comprising administering to the respiratory tract of a patient in need thereof an effective amount of a respirable dry powder of claim 1 .

21. A method for treating or reducing the incidence or severity of an acute exacerbation of a respiratory disease selected from the group consisting of COPD, chronic bronchitis, emphysema, asthma, cystic fibrosis, or non-cystic fibrosis bronchiectasis, comprising administering to the respiratory tract of a patient in need thereof an effective amount of a respirable dry powder of claim 1 .

22. The method of claim 20 , wherein the respiratory disease is COPD.

23. A dry powder inhaler that contains the receptacle of claim 1 , wherein the dry powder inhaler is a capsule-based dry powder inhaler or a blister-based dry powder inhaler.

Assignments (2)
CHANGE OF NAME Recorded Jun 28, 2017
From: PULMATRIX, INC.
To: PULMATRIX OPERATING COMPANY, INC.
Reel/Frame 043019/0117 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 5, 2016
From: SUNG, JEAN C.; MANZANEDO, DIANA; PERRY, JASON M.; DEHAAN, WESLEY; TRAUTMAN, BRIAN
To: PULMATRIX, INC.
Reel/Frame 037408/0564 →
Continuity (5)
Continuation PCTUS2014025660 · Mar 13, 2014
Provisional Application 61807063 · Apr 1, 2013
Provisional Application 61874146 · Sep 5, 2013
Provisional Application 61925400 · Jan 9, 2014
Related Publication 20160120855A1 · May 5, 2016