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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

The present invention provides new antibiotic compositions for use in mammalian eyes, particularly humans, to prevent, control or manage ocular microbial infections, reduce inflammation and pain, and prevent corneal injuries. The compositions include a quinolone component, an NSAID component, and a carrier component. The quinolone component has antifungal and bacteriocidal properties, while the NSAID component reduces inflammation and pain. The compositions are effective, safe, and can be used in single or multiple dose forms. The use of these compositions provides therapeutic benefits to humans or animals with ocular infections or injuries.

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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