Concentrated aqueous azalide formulations

Abstract

The present invention relates to formulations of concentrated azalide antibiotics and methods for making and using them. Specifically, the invention relates to a method of treating an infection comprising administering to a patient in need thereof, an effective amount of a concentrated aqueous azalide antibiotic formulation made according to the method comprising dissolving an azalide antibiotic in an aqueous solution comprising a strong acid. The invention also relates to methods for making concentrated aqueous azalide antibiotic formulations for use in pulmonary infection, a nasopharyngeal infection, an otic infection, an ocular infection, a dermal or a vaginal infection. The invention also relates to concentrated aqueous azalide antibiotic formulations made by dissolving an azalide antibiotic in an aqueous solution comprising a strong acid.

1 . A method of treating an infection comprising administering to a patient in need thereof, an effective amount of a concentrated aqueous azalide antibiotic formulation made according to the method comprising dissolving an azalide antibiotic in an aqueous solution comprising a strong acid. 
     
     
         2 . The method of  claim 1  wherein the azalide antibiotic is azithromycin. 
     
     
         3 . The method of  claim 2  wherein the aqueous azalide antibiotic formulation has about 2% to about 5% azithromycin. 
     
     
         4 . The method of  claim 2  wherein the aqueous azalide antibiotic formulation has about 3% azithromycin. 
     
     
         5 . The method of  claim 1  wherein the strong acid is hydrochloric acid. 
     
     
         6 . The method of  claim 1  wherein the aqueous solution has a pH of about 5 to about 6. 
     
     
         7 . The method of  claim 1  wherein the method further comprises the step of adding to the aqueous solution a second solution comprising a strong base. 
     
     
         8 . The method of  claim 7  wherein the strong base is sodium hydroxide. 
     
     
         9 . The method of  claim 7  wherein the second solution is added in an amount sufficient to bring the combined solutions to a pH from about 6 to about 7. 
     
     
         10 . The method of  claim 7  wherein the second solution is added in an amount sufficient to bring the combined solutions to a pH from about 6.3. 
     
     
         11 . The method of  claim 7  wherein the second solution comprises a polymeric agent. 
     
     
         12 . The method of  claim 11  wherein the polymeric agent is Noveon AA-1. 
     
     
         13 . The method of  claim 1  wherein the aqueous azalide antibiotic formulation comprises an anti-inflammatory agent. 
     
     
         14 . The method of  claim 16  wherein the anti-inflammatory agent is a dexamethasone. 
     
     
         15 . The method of  claim 14 , wherein the dexamethasone is at concentration of about 0.1%. 
     
     
         16 . The method of  claim 15  wherein the azalide antibiotic is azithromycin at a concentration of about 3%. 
     
     
         17 . The method of  claim 1  wherein the infection a pulmonary infection. 
     
     
         18 . The method of  claim 1  wherein the infection is a nasopharyngeal infection. 
     
     
         19 . The method of  claim 1  wherein the infection is an ocular infection. 
     
     
         20 . The method of  claim 1 , wherein the infection is a dermal infection. 
     
     
         21 . The method of  claim 1 , wherein the infection is an otic infection. 
     
     
         22 . A method of making a concentrated aqueous azalide antibiotic formulation comprising dissolving an azalide antibiotic in an aqueous solution comprising a strong acid. 
     
     
         23 . The method of  claim 22  wherein the method further comprises the step of adding to the aqueous solution a second solution comprising a strong base. 
     
     
         24 . A concentrated topical aqueous azalide antibiotic formulation made by the method comprising dissolving an azalide antibiotic in an aqueous solution comprising a strong acid. 
     
     
         25 . The formulation of  claim 24  wherein the method further comprises the step of adding to the aqueous solution a second solution comprising a strong base.