IP Library Granted Patent US 9,511,082
Granted Patent B2
US 9,511,082 · App. 15/205,918 · Granted Dec 6, 2016

Lipid-based compositions of antiinfectives for treating pulmonary infections and methods of use thereof

Inventor: Jeff Weers (Belmont, CA)
Assignee: INSMED INCORPORATED
A61K31/7036A61K9/0073A61K9/127A61M11/001A61M11/005A61M11/006A61M11/02A61M15/009A61M15/0091A61M15/08
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Quick Facts
Patent No.
US 9,511,082
App. No.
15/205,918
Granted
Dec 6, 2016
Kind
B2
Abstract

A system for treating or providing prophylaxus against a pulmonary infection is disclosed comprising: a) a pharmaceutical formulation comprising a mixture of free antiinfective and antiinfective encapsulated in a lipid-based composition, and b) an inhalation delivery device. A method for providing prophylaxis against a pulmonary infection in a patient and a method of reducing the loss of antiinfective encapsulated in a lipid-based composition upon nebulization comprising administering an aerosolized pharmaceutical formulation comprising a mixture of free antiinfective and antiinfective encapsulated in a lipid-based composition is also disclosed.

Claims (32)

1. A pharmaceutical formulation comprising a mixture of free quinolone antibiotic agent, a quinolone antibiotic agent encapsulated in a plurality of liposomes, and a pharmaceutical excipient, wherein the formulation is a solution or a suspension, the ratio by weight of the free quinolone antibiotic agent to the encapsulated quinolone antibiotic agent is between about 1:10 and about 10:1, and the lipid component of the plurality of liposomes consists of a phospholipid and a sterol.

2. The pharmaceutical formulation of claim 1 , wherein the free quinolone antibiotic agent is a fluoroquinolone and the quinolone antibiotic agent encapsulated in the plurality of liposomes is a fluoroquinolone.

3. The pharmaceutical formulation of claim 1 , wherein the free quinolone antibiotic agent and the quinolone antibiotic agent encapsulated in the plurality of liposomes is independently, ciprofloxacin, enoxacin, gatifloxacin, grepafloxacin, levofloxacin, lomefloxacin, moxifloxacin, nalidixic acid, norfloxacin, ofloxacin, sparfloxacin, trovafloxacin, oxolinic acid, gemifloxacin, or perfloxacin.

4. The pharmaceutical formulation of claim 1 , wherein the free quinolone antibiotic agent is ciprofloxacin and the quinolone antibiotic agent encapsulated in the plurality of liposomes is ciprofloxacin.

5. The pharmaceutical formulation of claim 1 , wherein the phospholipid is a phosphatidylcholine.

6. The pharmaceutical formulation of claim 5 , wherein the phosphatidylcholine is hydrogenated soy phosphatidylcholine (HSPC).

7. The pharmaceutical formulation of claim 5 , wherein the sterol is cholesterol.

8. The pharmaceutical formulation of claim 6 , wherein the sterol is cholesterol.

9. The pharmaceutical formulation of claim 1 , wherein the phospholipid is hydrogenated soy phosphatidylcholine (HSPC), the sterol is cholesterol, the free quinolone antibiotic agent is a fluoroquinolone and the quinolone antibiotic agent encapsulated in the plurality of liposomes is a fluoroquinolone.

10. The pharmaceutical formulation of claim 1 , wherein the phospholipid is a phosphatidylcholine, the free quinolone antibiotic agent is ciprofloxacin and the quinolone antibiotic agent encapsulated in the plurality of liposomes is ciprofloxacin.

11. The pharmaceutical formulation of claim 1 , wherein the phospholipid is a phosphatidylcholine, the sterol is a cholesterol, the free quinolone antibiotic agent is ciprofloxacin and the quinolone antibiotic agent encapsulated in the plurality of liposomes is ciprofloxacin.

12. The pharmaceutical formulation of claim 1 , wherein the phospholipid is a hydrogenated soy phosphatidylcholine (HSPC), the sterol is cholesterol, the free quinolone antibiotic agent is ciprofloxacin and the quinolone antibiotic agent encapsulated in the plurality of liposomes is ciprofloxacin.

13. The pharmaceutical formulation of claim 12 , wherein the formulation is an aerosol.

14. The pharmaceutical formulation of claim 1 , wherein the ratio by weight of free quinolone antibiotic agent to the encapsulated quinolone antibiotic agent is between about 1:2 and about 2:1.

15. The pharmaceutical formulation of claim 12 , wherein the ratio by weight of free ciprofloxacin to the encapsulated ciprofloxacin is between about 1:2 and about 2:1.

16. The pharmaceutical formulation of claim 15 , wherein the formulation is an aerosol.

17. A system for treating or providing prophylaxis against a pulmonary infection comprising:

a) the pharmaceutical formulation of claim 1 , and

b) an inhalation delivery device.

18. The system of claim 17 , wherein the inhalation delivery device is a nebulizer, the phospholipid is hydrogenated soy phosphatidylcholine (HSPC), the sterol is cholesterol, the free quinolone antibiotic agent is ciprofloxacin and the quinolone antibiotic agent encapsulated in the plurality of liposomes is ciprofloxacin.

19. The system of claim 18 , wherein the nebulizer is a single dose nebulizer.

20. A method for treating a pulmonary infection in a patient in need thereof comprising, nebulizing the pharmaceutical formulation of claim 1 , to generate a nebulized pharmaceutical formulation, administering the nebulized pharmaceutical formulation to the lungs of the patient.

21. A method for treating a pulmonary infection in a patient in need thereof comprising, nebulizing the pharmaceutical formulation of claim 11 , to generate a nebulized pharmaceutical formulation, administering the nebulized pharmaceutical formulation to the lungs of the patient.

22. A method for treating a pulmonary infection in a patient in need thereof comprising, nebulizing the pharmaceutical formulation of claim 12 , to generate a nebulized pharmaceutical formulation, administering the nebulized pharmaceutical formulation to the lungs of the patient.

23. A method for treating a pulmonary infection in a patient in need thereof comprising, nebulizing the pharmaceutical formulation of claim 15 , to generate a nebulized pharmaceutical formulation, administering the nebulized pharmaceutical formulation to the lungs of the patient.

24. The method of claim 20 , wherein the patient is a bronchiectasis patient.

25. The method of claim 21 , wherein the patient is a bronchiectasis patient.

26. The method of claim 22 , wherein the patient is a bronchiectasis patient.

27. The method of claim 23 , wherein the patient is a bronchiectasis patient.

28. The method of claim 22 , wherein the pulmonary infection is a Pseudomonas Aeruginosa infection.

29. The method of claim 23 , wherein the pulmonary infection is a Pseudomonas Aeruginosa infection.

30. The method of claim 26 , wherein the pulmonary infection is a Pseudomonas Aeruginosa infection.

Assignments (6)
PATENT SECURITY AGREEMENT Recorded Oct 20, 2022
From: INSMED INCORPORATED
To: BIOPHARMA CREDIT PLC
Reel/Frame 061735/0875 →
SECOND LIEN PATENT SECURITY AGREEMENT Recorded Oct 19, 2022
From: INSMED INCORPORATED
To: ORBIMED ROYALTY & CREDIT OPPORTUNITIES IV, LP
Reel/Frame 061727/0039 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 21, 2016
From: WEERS, JEFF
To: TRANSAVE, INC.
Reel/Frame 039214/0115 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 21, 2016
From: WEERS, JEFF
To: TRANSAVE, INC.
Reel/Frame 039214/0173 →
MERGER Recorded Jul 21, 2016
From: TRANSAVE, INC.
To: TRANSAVE, LLC
Reel/Frame 039214/0185 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 21, 2016
From: TRANSAVE, LLC
To: INSMED INCORPORATED
Reel/Frame 039214/0201 →
Continuity (7)
Continuation 14987508 · Jan 4, 2016
Continuation 14080922 · Nov 15, 2013
Continuation 13666420 · Nov 1, 2012
Continuation 13527213 · Jun 19, 2012
Continuation 11634343 · Dec 5, 2006
Provisional Application 60748468 · Dec 8, 2005
Related Publication 20160317563A1 · Nov 3, 2016