IP Library Granted Patent US 9,707,228
Granted Patent B2
US 9,707,228 · App. 14/402,060 · Granted Jul 18, 2017

Dry powder formulation

Inventors: Desmond Heng (Jurong Island, SG); Sie Huey Lee (Jurong Island, SG); Jeanette Teo (Singapore, SG); Wai Kiong Ng (Jurong Island, SG); Reginald Tan (Jurong Island, SG)
Assignees: Agency for Science, Technology and Research; National University Hospital
A61K31/496A61K9/0075A61K31/4375A61K31/4709A61K31/4745A61K31/5383A61K31/542A61K45/06
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Quick Facts
Patent No.
US 9,707,228
App. No.
14/402,060
Granted
Jul 18, 2017
Kind
B2
Abstract

A dry powder formulation comprising a combination of at least a first pharmaceutically active quinolone and a second pharmaceutically active quinolone.

Claims (20)

1. A dry powder formulation comprising a plurality of spray-dried particles, wherein each spray-dried particle is a binary combination consisting of a first pharmaceutically active quinolone and a second pharmaceutically active quinolone at a ratio of at least 1:2.

2. The dry powder formulation of claim 1 , wherein said ratio is selected to provide a synergistic effect on a microbial infection.

3. The dry powder formulation of claim 1 , wherein said first pharmaceutically active quinolone and said second pharmaceutically active quinolone is independently selected from a fluoroquinolone.

4. The dry powder formulation of claim 3 , wherein said fluoroquinolone is selected from the group consisting of ciprofloxacin, gatifloxacin, enoxacin, fleroxacin, lomefloxacin, nadifloxacin, norfloxacin, ofloxacin, pefloxacin, rufloxacin, balofloxacin, grepafloxacin, levofloxacin, pazufloxacin, sparfloxacin, temafloxacin, tosufloxacin, clinafloxacin, gemifloxacin, moxifloxacin, sitafloxacin, trovafloxacin, prulifloxacin and pharmaceutically acceptable salts thereof.

5. The dry powder formulation of claim 4 , wherein said first pharmaceutically active quinolone is ciprofloxacin and said second pharmaceutically active quinolone is gatifloxacin.

6. The dry powder formulation of claim 5 , wherein said first pharmaceutically active quinolone is ciprofloxacin hydrochloride and said second pharmaceutically active quinolone is gatifloxacin hydrochloride.

7. The dry powder formulation of claim 1 , wherein said first pharmaceutically active quinolone and said second pharmaceutically active quinolone are present in said formulation in the form of particles having a narrow particle size distribution.

8. The dry powder formulation of claim 7 , wherein said particles have a particle size between 500 nm to 4 μm.

9. The dry powder formulation of claim 7 , wherein said particles have a mono-modal size distribution with a span (D 90 −D 10 )/D 50 of 0.5 to 2.

10. The dry powder formulation of claim 7 , wherein said particles have a fine particle fraction in the range of 1% to 99%.

11. The dry powder formulation of claim 1 , wherein said dry powder formulation is for administration via a dry powder inhaler.

12. A method for preparing a dry powder formulation comprising the step of co-spray drying a binary system consisting of aqueous solutions of a first pharmaceutically active quinolone and a second pharmaceutically active quinolone to form spray-dried particles of the first pharmaceutically active quinolone and the second pharmaceutically active quinolone, wherein each spray-dried particle is a binary combination consisting of the first pharmaceutically active quinolone and the second pharmaceutically active quinolone at a ratio of at least 1:2.

13. The method of claim 12 , wherein said aqueous solutions are provided at a weight ratio of at least 1:2.

14. The method of claim 13 , wherein said aqueous solutions are aqueous solutions of ciprofloxacin hydrochloride and gatifloxacin hydrochloride that are provided at a weight ratio of 1:2.5.

15. A dry powder inhaler comprising a dry powder formulation having a plurality of spray-dried particles therein, wherein each spray-dried particle is a binary combination consisting of a first pharmaceutically active quinolone and a second pharmaceutically active quinolone at a ratio of at least 1:2.

16. The dry powder inhaler of claim 15 , wherein said dry powder inhaler disperses said dry powder formulation at a rate between 30 to 100 L/min.

17. The dry powder formulation of claim 1 for use in treating a bacterial infection or a respiratory tract infection in a patient.

18. The dry powder formulation of claim 17 , wherein said bacterial infection is caused by a bacteria having a genera selected from the group consisting of Pseudomonas, Escherichia, Haemophilus, Klebsiella, Legionella, Moraxella, Proteus, Acinetobacter, Staphylococcus, Streptococcus, Enterococcus, Mycobacterium, Corynebacterium and Mycoplasma.

19. The dry powder formulation of claim 18 , wherein said bacterial infection is caused by a bacteria selected from the group consisting of Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Legionella pneumophila, Moraxella catarrhalis, Proteus mirabilis, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphyloccus aureus, Streptococcus pneumoniae, Staphylococcus epidermis, Eterococcus faecalis , and Streptococcus pyogenes, Mycobacterium tuberculosis , non-tuberculous mycobacteria, Corynebacterium diphtheria and Mycoplasma pneumoniae.

20. A method of treating a bacterial infection or respiratory tract infection in a patient, comprising administering the dry powder formulation of claim 1 to the patient, wherein said bacterial infection or respiratory tract infection is selected from the group consisting of pharyngitis, epiglottitis, laryngitis tracheitis, bronchitis, bronchiolitis, pneumonia, and tuberculosis.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 26, 2015
From: NG, WAI KIONG; LEE, SIE HUEY; HENG, DESMOND; TAN, REGINALD
To: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
Reel/Frame 035264/0949 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 26, 2015
From: TEO, JEANNETTE
To: NATIONAL UNIVERSITY HOSPITAL
Reel/Frame 035265/0043 →
Priority Claims (1)
SG 201203712-3 · May 21, 2012 · national
Continuity (1)
Related Publication 20150132386A1 · May 14, 2015