Antimicrobial compositions

Abstract

The present invention relates to antimicrobial compositions and more specifically compositions of quinolone carboxylic acid derivatives. These compositions have improved solubility, stability, and tolerability. These compositions are useful for intravenous administration for treating, preventing, or reducing the risk of infection.

1 .- 97 . (canceled) 
     
     
         98 . A pharmaceutical composition comprising:
 (a) a quinolone carboxylic acid derivative or a pharmaceutically acceptable salt or ester thereof, wherein the quinolone carboxylic acid derivative corresponds to the following compound (A):   
       
         
           
           
               
               
           
         
         and 
         (b) a cyclodextrin; wherein the cyclodextrin is selected from a hydroxypropyl beta-cyclodextrin corresponding to the CAS Registry Number 128446-35-5 and a sulfobutyl ether beta-cyclodextrin corresponding to the CAS Registry Number 182410-00-0. 
       
     
     
         99 . The pharmaceutical composition according to  claim 98 , wherein the cyclodextrin is the hydroxypropyl beta-cyclodextrin corresponding to the CAS Registry Number 128446-35-5. 
     
     
         100 . The pharmaceutical composition according to  claim 98 , wherein the cyclodextrin is the sulfobutyl ether beta-cyclodextrin corresponding to the CAS Registry Number 182410-00-0. 
     
     
         101 . The pharmaceutical composition according to  claim 98 , wherein the quinolone carboxylic acid derivative is a D-glucitol, 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoro-2-pyridinyl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxy-1-azetidinyl)-4-oxo-3-quinolinecarboxylate (salt). 
     
     
         102 . The pharmaceutical composition according to  claim 98 , wherein the quinolone carboxylic acid derivative is D-glucitol, 1-deoxy-1-(methylamino)-,1-(6-amino-3,5-difluoro-2-pyridinyl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxy-1-azetidinyl)-4-oxo-3-quinolinecarboxylate trihydrate (salt). 
     
     
         103 . The pharmaceutical composition according to  claim 98  further comprising a chelating agent. 
     
     
         104 . The pharmaceutical composition according to  claim 103  wherein the chelating agent is disodium EDTA. 
     
     
         105 . The pharmaceutical composition according to  claim 98  further comprising a polyhydroxyamine compound. 
     
     
         106 . The pharmaceutical composition according to  claim 105 , wherein the polyhydroxyamine compound is meglumine. 
     
     
         107 . The pharmaceutical composition according to  claim 98 , wherein the quinolone carboxylic acid derivative has a measurable improvement in solubility compared to the quinolone carboxylic acid derivative in water, and/or the composition has improved stability, and/or the composition provides a measurable enhancement in venous toleration. 
     
     
         108 . A pharmaceutical composition comprising:
 (a) from about 100 mg to about 500 mg of delafloxacin meglumine,   (b) from about 15 mg to about 125 mg meglumine,   (c) from about 500 mg to about 5000 mg of sulfobutyl ether beta-cyclodextrin corresponding to the CAS Registry Number 182410-00-0; and   (d) from 0 mg to about 4 mg disodium EDTA.   
     
     
         109 . The pharmaceutical composition according to  claim 108  which is in the form of a lyophile. 
     
     
         110 . A method of treating, preventing, or reducing the risk of a bacterial infection comprising administering to a patient in need thereof a composition according to  claim 98 . 
     
     
         111 . The method according to  claim 110 , wherein the bacterial infection is a methicillin-resistant  Staphylococcus aureus  infection.