Compositions including antibiotics and methods for using same

a technology of antibiotics and compositions, applied in the field of compositions including antibiotics, can solve the problems of affecting the antibacterial effect, so as to improve the antifungal and bacteriocidal properties, prevent, control or manage, and maintain the effect of sufficiency preservative activity

Inactive Publication Date: 2008-03-20
ALLERGAN INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0008] The present compositions preferably have added protection against microbial, for example, fungal contamination. This feature provides added assurance to the user that the present compositions are free of detrimental microbial contamination. This feature may allow reduced concentrations of preservatives to be included in the present compositions, thereby advantageously reducing detrimental side effects caused by such preservatives when the compositions are administered to patients. The present compositions can be easily produced, for example, using conventional techniques and can be conveniently used, for example, employing conventional methods of administration.
[0009] In accordance with one aspect of the invention, the compositions comprise a quinolone component, a NSAID component and a carrier component. The quinolone component is present in an amount effective as a antibiotic when the composition is placed in a mammalian eye. In one useful embodiment, the quinolone component in the composition has fungistatic activity. That is, the quinolone components in the present compositions have sufficient anti-fungal properties or activity to substantially prevent increases in populations of fungi in such compositions. In effect, the present quinolone components act as effective preservatives against fungal growth or contamination in the present compositions. The fungistatic activity of the presently useful quinolone components in the present compositions provide benefits, for example, as described elsewhere herein, which are surprising and substantial. The NSAID component is present in an amount effective to reduce at least one of inflammation and pain when the composition is placed in a mammalian eye. The carrier component is present in an amount effective to act as a carrier for the quinolone component and the NSAID component in the composition, and preferably is ophthalmically acceptable.
[0015] In both single and multiple use dosage forms the ability of the present compositions to maintain suffficent preservative activity during storage and after opening the package is an advantage of the quinolone component's useful antifungal and bacteriocidal and / or bacteriostatic properties.
[0016] Methods of using these compositions are included in the scope of the present invention. Such methods comprise administering to a human or animal, preferably to a mammalian eye, a therapeutically effective amounts of the compositions as described herein. Such methods provide one or more benefits to the human or animal treated in accordance with the present methods. For example, such benefits include prevention, control or management of microbial infections, and reduction in inflammation and / or pain.
[0017] In another aspect of the present invention, methods for treating corneal injuries are provided. As used herein, the term “corneal injury” refers to an injury of the cornea which is infected by harmful and / or unwanted microorganism or which, if left untreated is likely to become so infected, for example, before this injury heals. A corneal ulcer is an example of a corneal injury. Such methods comprise administering to a mammalian eye having a corneal injury a therapeutically effective amount of a composition comprising a quinolone component in an amount effective as an antibiotic in the mammalian eye and a NSAID component in an amount effective, in combination with the quinolone component, to provide a reduction in pain caused by the corneal injury. Such reduction in pain, together with the antibiotic effectiveness of the presently useful compositions, reduces the discomfort to the patient resulting from the corneal injury and facilitates or promotes the healing of the injury. The present useful compositions preferably include a carrier component in an amount effective to act as a carrier for the quinolone component and the NSAID component in the presently useful composition.
[0018] In another aspect of the present invention, methods for treating ocular infections, such as corneal infections and the like, are provided. Such methods comprise administering to a mammalian eye having an infection caused by one or more microbes or pathogens a therapeutically effective amount of a composition comprising a quinolone component in an amount effective as an antibiotic in the mammalian eye and an effective amount of a NSAID component. In one embodiment, the NSAID component is present in an amount effective to reduce the time needed to eliminate the infection relative to identically administering a similar composition without the NSAID component. In a particularly preferred embodiment the NSAID is bromfenac. The administering step preferably is effective to at least inhibit the offending microbe(s) or pathogen(s) from adhering to a surface of the mammalian eye and / or to inhibit colonization of the offending microbe(s) or pathogen(s) in the mammalian eye.

Problems solved by technology

Antibiotic compositions, even with preservatives, have been susceptible to microbial, for example, fungal, contamination.
In addition, preservatives tend to cause irritation, allergic reactions, and / or other detrimental side effects when the preserved composition is administered to a patient.
Corneal injuries, such as corneal ulcers and other corneal conditions which are infected or if left untreated are likely to become infected, are quite painful and sometimes require lengthy periods of time to heal.

Method used

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  • Compositions including antibiotics and methods for using same

Examples

Experimental program
Comparison scheme
Effect test

examples 1 to 11

[0068] A series of compositions, Compositions 1 to 11, are prepared by blending various components together. These compositions have the following chemical make-ups.

Composition 1Ofloxacin0.6w / v %NaCl0.79w / v %pH6.4q.s. 100%Composition 2Moxifloxacin0.1w / v %NaCl0.79w / v %pH6.4q.s. 100%Composition 3Ofloxacin0.6w / v %NaCl0.3w / v %EDTA0.1wt %Boric Acid1.0w / v %pH6.4q.s. 100%Composition 4Moxifloxacin0.1w / v %NaCl0.3w / v %EDTA0.1w / v %Boric Acid1.0w / v %pH6.4q.s. 100%Composition 5Bromfenac0.1w / v %Ofloxacin0.6w / v %NaCl0.79w / v %pH6.4q.s. 100%Composition 6Bromfenac0.1w / v %Ofloxacin1.0w / v %NaCl0.79w / v %pH6.4q.s. 100%Composition 7Ketorolac0.5w / v %Moxifloxacin0.5w / v %NaCl0.3w / v %EDTA0.1w / v %Boric Acid1.0w / v %pH6.4q.s. 100%Composition 8Bromfenac0.1w / v %Moxifloxacin0.5w / v %NaCl0.3w / v %EDTA0.1w / v %Boric Acid1.0w / v %pH6.4q.s. 100%Composition 9Bromfenac0.1w / v %Ofloxacin0.3w / v %NaCl0.79w / v %BAK0.005w / v %L-Arginine0.28w / v %pH6.4q.s. 100%Composition 10Bromfenac0.1w / v %Moxifloxacin0.3w / v %NaCl0.79w / v %BAK0.005w...

examples 12 to 23

[0073] A further series of compositions, Compositions 12 to 24, are prepared by blending various components together. These compositions have the following chemical make-ups. Each composition included sufficient water to total 100% by weight.

EXAMPLECONCENTRATION,NO.COMPOSITIONw / v %12Bromfenac0.1Ofloxacin0.3NaCl0.79pH6.413Bromfenac0.1Ofloxacin0.3NaCl0.30EDTA0.1Boric Acid1.0pH6.414Bromfenac0.1Ofloxacin0.3NaCl0.79BAK0.005pH6.415Bromfenac0.5Ofloxacin0.3NaCl0.79pH7.416Ketorolac0.1Ofloxacin0.3NaCl0.79BAK0.005pH7.617Bromfenac0.1Ofloxacin0.3NaCl0.79BAK0.005Octoxynol (3)0.007pH6.418Bromfenac0.1Ofloxacin0.3NaCl0.79BAK0.005Octoxynol (3)0.007pH7.619Bromfenac0.1Ofloxacin0.3NaCl0.79BAK0.005Cyclodextrin (4)0.1pH6.420Bromfenac0.1Ofloxacin0.5NaCl0.79BAK0.005Cyclodextrin (4)0.1pH7.621Bromfenac0.1Ofloxacin0.3NaCl0.79Purite (5)0.007pH7.622Bromfenac0.1Ofloxacin0.3NaCl0.79Purite (5)0.007Octoxynol (3)0.007pH7.623Bromfenac0.1Ofloxacin0.3NaCl0.79Purite (5)0.007Cyclodextrin (4)0.1pH7.6

(3) Polyethylene glyc...

examples 24 to 41

[0078] Compositions 5 to 10 and 12 to 23 are each administered to a human eye which has been subjected to surgical trauma. Before administration, each eye exhibits a degree of inflammation and is the source of a degree of pain.

[0079] Each composition in the form of a solution is administered to the eye in an amount of about 1 to 2 drops per eye with the drops containing about 25 to 50 micro liters. The drops are administered 3 to 4 times per day. Each composition in the form of a gel is administered by placing about 50 to 100 microliters of the composition between the eyelid and the eyeball 3 to 4 times a day.

[0080] After a week of such administering, each of the eyes treated exhibits no inflammation and is not a source of pain. In addition, each of the eyes has remained free of microbial infection.

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Abstract

Compositions including a quinolone component, such as ofloxacin, having fungistatic activity in the compositions, present in an amount effective as an antibiotic when the composition is placed in a mammalian eye, a NSAID component present in an amount to reduce inflammation or pain when the composition is placed in the eye, and a carrier component in an amount effective to act as a carrier for the quinolone component and NSAID component are provided. Methods of using the present compositions, for example, to resolve microbial infections and / or to reduce inflammation and / or pain in a mammalian eye are included within the scope of the present invention. Methods for treating corneal injuries are also included. In addition, methods for treating ocular infections, for example, corneal infections, are included.

Description

RELATED APPLICATION [0001] This application is a continuation-in-part of co-pending U.S. patent application Ser. No. 10 / 236,712, filed Sep. 6, 2002, which is a continuation of U.S. patent application Ser. No. 09 / 624,129, filed Jul. 14, 2000, which is a continuation-in-part of U.S. patent application Ser. No. 09 / 364,334 filed Jul. 30, 1999, and U.S. patent application Ser. No. 09 / 365,291, filed Jul. 30, 1999, the disclosure of each of which is hereby incorporated in its entirety herein by reference.BACKGROUND OF THE INVENTION [0002] The present invention relates to compositions including antibiotics and to methods for using such compositions. More particularly, the invention relates to compositions including antibiotics which have added protection against fungal contamination, which reduce inflammation or pain and / or which are useful in the treatment of corneal ulcers. [0003] Various antibiotic components have been used in ocular applications, for example, to control or manage or pre...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/196A61K31/5365A61P27/02A61P29/00A61K31/192A61K45/00A61K31/407A61K31/47A61K31/495A61K31/496A61K31/535A61K31/5383A61P31/04A61P31/10A61P43/00
CPCA61K9/0048A61K31/196A61K31/535A61K31/5365Y10S514/912A61K31/40A61K2300/00A61P27/02A61P29/00A61P31/04A61P31/10A61P43/00
Inventor MULLER, CHRISTOPHER A.BANCROFT, ELIZABETH A.CHEETHAM, JANET K.JENSEN, HAROLD G.KUAN, TERESA H.POWER, DAVID F.SKULE, KEVIN D.
Owner ALLERGAN INC
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