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WO2007070413A1 - Treatment of corneal ulcers with topical gatifloxacin - Google Patents

Treatment of corneal ulcers with topical gatifloxacin Download PDF

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Publication number
WO2007070413A1
WO2007070413A1 PCT/US2006/046990 US2006046990W WO2007070413A1 WO 2007070413 A1 WO2007070413 A1 WO 2007070413A1 US 2006046990 W US2006046990 W US 2006046990W WO 2007070413 A1 WO2007070413 A1 WO 2007070413A1
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WO
WIPO (PCT)
Prior art keywords
gatifloxacin
topical
treatment
corneal ulcers
ciprofloxacin
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2006/046990
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French (fr)
Inventor
Harold G. Jensen
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Allergan Inc
Original Assignee
Allergan Inc
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Filing date
Publication date
Application filed by Allergan Inc filed Critical Allergan Inc
Publication of WO2007070413A1 publication Critical patent/WO2007070413A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents

Definitions

  • a method comprising topically administering an effective amount of gatifloxacin to an eye of a mammal for the treatment of bacterial corneal ulcers.
  • Another embodiment is use of gatifloxacin in the manufacture of a medicament for the treatment of bacterial corneal ulcers in a mammal.
  • the bacterial corneal ulcer is caused by a gram positive bacteria.
  • the bacterial corneal ulcer is caused by Streptococcus pneumoniae.
  • the concentration of gatifloxacin is from about 0.03% (w/v) to 3% (w/v).
  • the concentration of gatifloxacin is about 0.3% (w/v).
  • Zymar ® is a 0.3% (w/v) ophthalmic solution available from Allergan, Inc. that is , useful for the methods disclosed herein.
  • topical gatifloxacin is administered once a day.
  • topical gatifloxacin is administered twice a day.
  • topical gatifloxacin is administered three times a day.
  • topical gatifloxacin is administered four times a day.
  • topical gatifloxacin is administered five times a day.
  • topical gatifloxacin is administered as needed.
  • Results The most common organisms isolated were Streptococcus pneumoniae (42/73; 57.5%) and Pseudomonas aeruginosa (12/73; 16.4%).41 out of 42 culture samples (97.6%) with Streptococcus pneumoniae isolates were susceptible to gatifloxacin (MIC90: 0.75 ⁇ g/mL), compared with 5 out of 42 samples (11.9%) that were susceptible to ciprofloxacin (MIC90: 4 ⁇ g/mL).
  • Gatifloxacin and ciprofloxacin exhibited high antimicrobial efficacy against gram negative organisms. Because of its broader spectrum of coverage, it is likely that gatifloxacin will be a better initial therapy than ciprofloxacin for acute bacterial corneal ulcers.

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  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Ophthalmology & Optometry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Therapeutic methods for the treatment of bacterial corneal ulcers and medicaments of gatifloxacin for topical administration are disclosed herein.

Description

17881 (AP) TREATMENT OF CORNEAL ULCERS WITH TOPICAL GATIFLOXACIN
Description of the Invention
[0001] Disclosed herein is a method comprising topically administering an effective amount of gatifloxacin to an eye of a mammal for the treatment of bacterial corneal ulcers.
[0002] Another embodiment is use of gatifloxacin in the manufacture of a medicament for the treatment of bacterial corneal ulcers in a mammal.
[0003] In another embodiment, the bacterial corneal ulcer is caused by a gram positive bacteria.
[0004] In another embodiment, the bacterial corneal ulcer is caused by Streptococcus pneumoniae.
[0005] In another embodiment the concentration of gatifloxacin is from about 0.03% (w/v) to 3% (w/v).
[0006] In another embodiment the concentration of gatifloxacin is about 0.3% (w/v). [0007] Zymar® is a 0.3% (w/v) ophthalmic solution available from Allergan, Inc. that is , useful for the methods disclosed herein.
[0008] In one embodiment, topical gatifloxacin is administered once a day. [0009] In another embodiment, topical gatifloxacin is administered twice a day. [00010] In another embodiment, topical gatifloxacin is administered three times a day.
[00011] In another embodiment, topical gatifloxacin is administered four times a day.
[00012] In another embodiment, topical gatifloxacin is administered five times a day.
[00013] In another embodiment, topical gatifloxacin is administered as needed.
Example
[00014] Purpose: To compare the effect of gatifloxacin 0.3% and ciprofloxacin
0.3% on bacterial isolates taken from patients with acute bacterial corneal ulcers. [00015] Methods: 75 patients were enrolled into a multicenter, investigator- masked, clinical comparison of gatifloxacin 0.3% and ciprofloxacin 0.3% in the treatment of acute bacterial corneal ulcers. Microbiological culture samples were obtained from the area of ulceration before treatment to evaluate the type of organisms present and susceptibility to antibiotics. 72 and 73 culture samples were available to test the susceptibility to gatifloxacin and ciprofloxacin respectively. [00016] Results: The most common organisms isolated were Streptococcus pneumoniae (42/73; 57.5%) and Pseudomonas aeruginosa (12/73; 16.4%).41 out of 42 culture samples (97.6%) with Streptococcus pneumoniae isolates were susceptible to gatifloxacin (MIC90: 0.75 μg/mL), compared with 5 out of 42 samples (11.9%) that were susceptible to ciprofloxacin (MIC90: 4 μg/mL). A slightly smaller percentage of Pseudomonas aeruginosa isolates were susceptible to gatifloxacin [83.3% (10/12); MIC90: 3 μg/mL], and ciprofloxacin: [91.7% (11/12); MIC90: 1 μg/mL). A total of 93.1% (67/72) of all organisms were susceptible to gatifloxacin (MIC90: 2 μg/mL), while 38.4% (28/73) were susceptible to ciprofloxacin (MIC90: 4 μg/mL). Similarly, 94.4% (51/54) of all gram positive organisms were susceptible to gatifloxacin (MIC90: 1 μg/mL) while 20.4% (11/54) were susceptible to ciprofloxacin (MIC90: 4 μg/mL); 88.9% (16/18) of all gram negative organisms were susceptible to gatifloxacin (MEC90: 3 μg/mL) while 89.5% (17/19) were susceptible to ciprofloxacin (MIC90: 2 μg/mL). [00017] Conclusion: Gatifloxacin exhibited greater antimicrobial efficacy than ciprofloxacin against gram positive organisms in general and Streptococcus pneumoniae, specifically. Gatifloxacin and ciprofloxacin exhibited high antimicrobial efficacy against gram negative organisms. Because of its broader spectrum of coverage, it is likely that gatifloxacin will be a better initial therapy than ciprofloxacin for acute bacterial corneal ulcers.

Claims

What is claimed is:
1. Use of gatifloxacϊn in the manufacture of a medicament for the treatment of bacterial corneal ulcers in a mammal.
2. Use of claim 1, wherein the bacterial corneal ulcer is caused by a gram positive bacteria.
3. Use of claim 1, the bacterial corneal ulcer is caused by Streptococcus pneumoniae.
4. Use of any one of claims 1 to 3 wherein the concentration of gatifloxacin is from about 0.03% (w/v) to 3% (w/v).
5. Use of any one of claims 1 to 4 wherein the concentration of gatifloxacin is about 0.3% (w/v).
PCT/US2006/046990 2005-12-12 2006-12-11 Treatment of corneal ulcers with topical gatifloxacin Ceased WO2007070413A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US75001705P 2005-12-12 2005-12-12
US60/750,017 2005-12-12

Publications (1)

Publication Number Publication Date
WO2007070413A1 true WO2007070413A1 (en) 2007-06-21

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PCT/US2006/046990 Ceased WO2007070413A1 (en) 2005-12-12 2006-12-11 Treatment of corneal ulcers with topical gatifloxacin

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WO (1) WO2007070413A1 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013002898A1 (en) * 2011-06-28 2013-01-03 Chevron U.S.A. Inc. System and method for generating a geostatistical model of a geological volume of interest that is constrained by a process-based model of the geological volume of interest

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005000307A1 (en) * 2003-06-26 2005-01-06 Santen Pharmaceutical Co., Ltd. Ophthalmic composition containing quinolones and method of use
CN1562030A (en) * 2004-04-20 2005-01-12 沈阳药科大学 Gatiflxacin eye gels based on HPMC medium and its preparing method

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005000307A1 (en) * 2003-06-26 2005-01-06 Santen Pharmaceutical Co., Ltd. Ophthalmic composition containing quinolones and method of use
CN1562030A (en) * 2004-04-20 2005-01-12 沈阳药科大学 Gatiflxacin eye gels based on HPMC medium and its preparing method

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
DATABASE WPI Week 200532, Derwent World Patents Index; AN 2005-306958, XP002426213 *
DONNENFELD E D ET AL: "PROPHYLAXIS OF STREPTOCOCCUS PNEUMONIAE KERATITIS WITH GATIFLOXACIN IN A RABBIT LASIK MODEL", ARVO ANNUAL MEETING ABSTRACT SEARCH AND PROGRAM PLANNER, vol. 2003, 2003, & ANNUAL MEETING OF THE ASSOCIATION FOR RESEARCH IN VISION AND OPHTHALMOLOGY; FORT LAUDERDALE, FL, USA; MAY 04-08, 2003, pages Abstract No. 4745, XP009080909 *
HSU V J ET AL: "Streptococcus mitis corneal ulcer", IOVS, vol. 46, no. Suppl. S, 2005, & ANNUAL MEETING OF THE ASSOCIATION-FOR-RESEARCH-IN-VISION-AND-OPHTHALM OLOGY; FT LAUDERDALE, FL, USA; MAY 01 -05, 2005, pages 2632, XP009080886, ISSN: 0146-0404 *
JENSEN HAROLD ET AL: "Comparison of ophthalmic gatifloxacin 0.3% and ciprofloxacin 0.3% in healing of corneal ulcers associated with Pseudomonas aeruginosa-induced ulcerative keratitis in rabbits", JOURNAL OF OCULAR PHARMACOLOGY AND THERAPEUTICS, vol. 21, no. 1, February 2005 (2005-02-01), pages 36 - 43, XP009081003, ISSN: 1080-7683 *
KOWALSKI R P ET AL: "Gatifloxacin and moxifloxacin: an in vitro susceptibility comparison to levofloxacin, ciprofloxacin, and ofloxacin using bacterial keratitis isolates", AMERICAN JOURNAL OF OPHTHALMOLOGY, OPHTHALMIC PUBL., CHICAGO, IL,, US, vol. 136, no. 3, September 2003 (2003-09-01), pages 500 - 505, XP004603216, ISSN: 0002-9394 *
MILLER J J ET AL: "Endophthalmitis caused by streptococcus pneumoniae", AMERICAN JOURNAL OF OPHTHALMOLOGY, OPHTHALMIC PUBL., CHICAGO, IL,, US, vol. 138, no. 2, August 2004 (2004-08-01), pages 231 - 236, XP004723185, ISSN: 0002-9394 *
MORRISSEY IAN ET AL: "Surveillance of the susceptibility of ocular bacterial pathogens to the fluoroquinolone gatifloxacin and other antimicrobials in Europe during 2001/2002.", THE JOURNAL OF INFECTION AUG 2004, vol. 49, no. 2, August 2004 (2004-08-01), pages 109 - 114, XP002426209, ISSN: 0163-4453 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013002898A1 (en) * 2011-06-28 2013-01-03 Chevron U.S.A. Inc. System and method for generating a geostatistical model of a geological volume of interest that is constrained by a process-based model of the geological volume of interest

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