IP Library Granted Patent US 10,987,357
Granted Patent B2
US 10,987,357 · App. 16/250,520 · Granted Apr 27, 2021

Aerosolized fluoroquinolones and uses thereof

Inventors: Mark W. Surber (San Diego, CA); Keith A. Bostian (Atherton, CA); Michael N. Dudley (San Diego, CA); Olga Rodny (Mill Valley, CA); David C. Griffith (San Marcos, CA)
Assignee: Horizon Orphan, LLC
A61K31/5383A61K9/0073A61K9/0078A61K9/5123A61K47/02A61K9/0075Y02A50/30
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Quick Facts
Patent No.
US 10,987,357
App. No.
16/250,520
Granted
Apr 27, 2021
Kind
B2
Abstract

Disclosed herein are formulations of fluoroquinolones suitable for aerosolization and use of such formulations for aerosol administration of fluoroquinolone antimicrobials for the treatment of pulmonary bacterial infections. In particular, inhaled levofloxacin specifically formulated and delivered for bacterial infections of the lungs is described. Methods include inhalation protocols and manufacturing procedures for production and use of the compositions described.

Claims (16)

1. A method of treating a bacterial lung infection, comprising administering a pharmaceutical aerosol for nasal, sinunasal or pulmonary administration comprising a dispersed liquid phase and a continuous gas phase, wherein the dispersed liquid phase:

(a) consists essentially of aqueous droplets comprising an active compound comprising levofloxacin, and at least one excipient comprising a divalent metal ion;

(b) has a mass median diameter from about 1 to about 5 μm; and

(c) has a droplet size distribution exhibiting a geometrical standard deviation less than or equal to 3.0 μm.

2. The method of claim 1 , wherein the lung infection is caused by one or more of the following bacteria: Pseudomonas aeruginosa, Pseudomonas fluorescens, Pseudomonas acidovorans, Pseudomonas alcaligenes, Pseudomonas putida, Stenotrophomonas maltophilia, Aeromonas hydrophilia, Escherichia coli, Citrobacter freundii, Salmonella typhimurium, Salmonella typhi, Salmonella paratyphi, Salmonella enteritidis, Shigella dysenteriae, Shigella flexneri, Shigella sonnei, Enterobacter cloacae, Enterobacter aerogenes, Klebsiella pneumoniae, Klebsiella oxytoca, Serratia marcescens, Morganella morganii, Proteus mirabilis, Proteus vulgaris, Providencia alcalifaciens, Providencia rettgeri, Providencia stuartii, Acinetobacter calcoaceticus, Acinetobacter haemolyticus, Yersinia enterocolitica, Yersinia pestis, Yersinia pseudotuberculosis, Yersinia intermedia, Bordetella pertussis, Bordetella parapertussis, Bordetella bronchiseptica, Haemophilus influenzae, Haemophilus parainfluenzae, Haemophilus haemolyticus, Haemophilus parahaemolyticus, Haemophilus ducreyi, Pasteurella multocida, Pasteurella haemolytica, Helicobacter pylori, Campylobacter fetus, Campylobacter jejuni, Campylobacter coli, Borrelia burgdorferi, Vibrio cholera, Vibrio parahaemolyticus, Legionella pneumophila, Listeria monocytogenes, Neisseria gonorrhoeae, Neisseria meningitidis, Burkholderia cepacia, Francisella tularensis, Kingella , and Moraxella.

3. The method of claim 2 , wherein the lung infection is caused by one or more of the following bacteria: Pseudomonas aeruginosa, Stenotrophomonas maltophilia, Haemophilus influenzae, Burkholderia cepacia , and Moraxella.

4. The method of claim 1 , wherein the lung infection is caused by a Mycobacterium bacteria.

5. The method of claim 4 , wherein the lung infection is caused by one or more bacteria selected from the group consisting of Mycobacterium tuberculosis, Mycobacterium avium, Mycobacterium intracellulare , and Mycobacterium leprae.

6. The method of claim 1 , wherein about 20 mg of levofloxacin is administered to the lung.

7. The method of claim 6 , wherein about 100 mg of levofloxacin is administered to the lung.

8. The method of claim 7 , wherein about 125 mg of levofloxacin is administered to the lung.

9. The method of claim 8 , wherein about 150 mg of levofloxacin is administered to the lung.

10. The method of claim 1 , wherein the aerosol is administered to the lung in less than 10 minutes.

11. The method of claim 10 , wherein the aerosol is administered to the lung in less than 5 minutes.

12. The method of claim 11 , wherein the aerosol is administered to the lung in less than 3 minutes.

13. The method of claim 12 , wherein the aerosol is administered to the lung in less than 2 minutes.

Assignments (7)
MERGER AND CHANGE OF NAME Recorded Dec 21, 2023
From: HORIZON THERAPEUTICS, LLC; HORIZON ORPHAN LLC
To: HORIZON THERAPEUTICS U.S. HOLDING LLC
Reel/Frame 065928/0608 →
RELEASE OF SECURITY INTEREST Recorded Oct 6, 2023
From: CITIBANK, N.A.
To: HORIZON THERAPEUTICS U.S. HOLDING LLC (FKA HORIZON ORPHAN LLC); HZNP LIMITED; HORIZON THERAPEUTICS U.S. HOLDING LLC (SUCCESSOR IN INTEREST TO HORIZON THERAPEUTICS, LLC)
Reel/Frame 065154/0041 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 28, 2021
From: MPEX PHARMACEUTICALS, INC.
To: TRIPEX PHARMACEUTICALS, LLC
Reel/Frame 056383/0920 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 28, 2021
From: TRIPEX PHARMACEUTICALS, LLC
To: RAPTOR PHARMACEUTICALS INC.
Reel/Frame 056422/0235 →
CHANGE OF NAME Recorded May 28, 2021
From: RAPTOR PHARMACEUTICALS INC.
To: HORIZON ORPHAN LLC
Reel/Frame 056424/0102 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 27, 2021
From: SURBER, MARK W; BOSTIAN, KEITH A; DUDLEY, MICHAEL N; LOMOVSKAYA, OLGA; GRIFFITH, DAVID C
To: MPEX PHARMACEUTICALS, INC.
Reel/Frame 056377/0274 →
SECURITY AGREEMENT Recorded Aug 17, 2020
From: HORIZON ORPHAN LLC; HORIZON THERAPEUTICS, LLC; HZNP LIMITED
To: CITIBANK, N.A.
Reel/Frame 053515/0273 →