Formulations for parenteral delivery of compounds and uses thereof

Abstract

The present invention provides formulations that achieve effective delivery of methylnaltrexone compositions. The provided formulations are useful for preventing, treating delaying, diminishing or reducing the severity of side effects resulting from use of analgesic opioids.

1 - 70 . (canceled) 
     
     
         71 . A pharmaceutical composition comprising:
 an aqueous solution of methylnaltrexone, or a pharmaceutically acceptable salt thereof, wherein the aqueous solution further comprises a calcium salt, a chelating agent, and a stabilizing agent that inhibits degradation of the methylnaltrexone in the solution into a compound of Formula (I),   
       
         
           
           
               
               
           
         
       
       at room temperature,
 wherein the methylnaltrexone is methylnaltrexone bromide provided at a concentration of about 5 mg/mL to about 32 mg/mL. 
 
     
     
         72 . The pharmaceutical composition of  claim 71 , wherein the stabilizing agent is glycine, benzoic acid, citric acid, glycolic acid, lactic acid, malic acid, or maleic acid. 
     
     
         73 . The pharmaceutical composition of  claim 72 , wherein the stabilizing agent is glycine, provided at a concentration within the range of about 0.1 mg/mL to about 0.8 mg/mL. 
     
     
         74 . The pharmaceutical composition of  claim 73 , wherein the stabilizing agent is glycine-HCl. 
     
     
         75 . The pharmaceutical composition of  claim 71 , wherein the chelating agent is a calcium salt chelating agent provided at a concentration of about 0.1 mg/mL to about 1.0 mg/mL. 
     
     
         76 . The pharmaceutical composition of  claim 72 , wherein the chelating agent is a calcium salt chelating agent provided at a concentration of about 0.1 mg/mL to about 1.0 mg/mL. 
     
     
         77 . The pharmaceutical composition of  claim 73 , wherein the chelating agent is a calcium salt chelating agent provided at a concentration of about 0.1 mg/mL to about 1.0 mg/mL. 
     
     
         78 . The pharmaceutical composition of  claim 74 , wherein the chelating agent is a calcium salt chelating agent provided at a concentration of about 0.1 mg/mL to about 1.0 mg/mL. 
     
     
         79 . The pharmaceutical composition of  claim 71 , wherein the calcium salt chelating agent is calcium disodium ethylenediaminetetraacetic acid (EDTA). 
     
     
         80 . The pharmaceutical composition of  claim 72 , wherein the calcium salt chelating agent is calcium disodium ethylenediaminetetraacetic acid (EDTA). 
     
     
         81 . The pharmaceutical composition of  claim 73 , wherein the calcium salt chelating agent is calcium disodium ethylenediaminetetraacetic acid (EDTA). 
     
     
         82 . The pharmaceutical composition of  claim 74 , wherein the calcium salt chelating agent is calcium disodium ethylenediaminetetraacetic acid (EDTA).