Process for producing injectable gabapentin compositions

Abstract

Injectable compositions containing gabapentin and processes for preparing sterile injectable compositions containing gabapentin are discussed. The process includes subjecting the compositions to heat. Heating results in increased production of gabapentin lactam, which has previously been shown to be toxic. Surprisingly, heated injectable compositions containing gabapentin are found to be non-toxic when administered intrathecally. Thus, heating for the purposes of sterilization or to assure sterility provides a viable option in the production of injectable compositions containing gabapentin.

1 . A process for preparing an injectable pharmaceutical composition comprising gabapentin, the process comprising: 
 preparing an injectable composition comprising gabapentin and a pharmaceutically acceptable vehicle; and    heating the injectable composition to an F 0  equivalent of about 1 or greater to produce the injectable pharmaceutical composition.    
   
   
       2 . The process of  claim 1 , wherein the injectable composition is heated to an F 0  equivalent of about 2 or greater.  
   
   
       3 . The process of  claim 2 , wherein the injectable composition is heated to an F 0  equivalent of about 3 or greater.  
   
   
       4 . The process of  claim 3 , wherein the injectable composition is heated to an F 0  equivalent of about 4 or greater.  
   
   
       5 . The process of  claim 4 , wherein the injectable composition is heated to an F 0  equivalent of about 8 or greater.  
   
   
       6 . The process of  claim 5 , wherein the injectable composition is heated to an F 0  equivalent of about 12 or greater.  
   
   
       7 . The process of  claim 6 , wherein the injectable composition is heated to an F 0  equivalent of about 18 or greater.  
   
   
       8 . The process of  claim 7 , wherein the injectable composition is heated to an F 0  equivalent of about 24 or greater.  
   
   
       9 . The process of  claim 1 , wherein the injectable pharmaceutical composition comprises less than or equal to about 10% (w/v) gabapentin lactam.  
   
   
       10 . The process of  claim 9 , wherein the injectable pharmaceutical compositioncomprises less than or equal to about 5% (w/v) gabapentin lactam.  
   
   
       11 . The process of  claim 10 , wherein the injectable pharmaceutical composition comprises less than or equal to about 2% (w/v) gabapentin lactam.  
   
   
       12 . The process of  claim 11 , wherein the injectable pharmaceutical composition comprises less than or equal to about 1% (w/v) gabapentin lactam.  
   
   
       13 . The process of  claim 1 , wherein the injectable pharmaceutical composition comprises between about 0.5% (w/v) and about 10% (w/v) gabapentin lactam.  
   
   
       14 . The process of  claim 1 , wherein the injectable pharmaceutical composition comprises between about 0.1 mg/ml and about 100 mg/ml gabapentin.  
   
   
       15 . The process of  claim 14 , wherein the injectable pharmaceutical composition comprises between about 30 mg/ml to about 100 mg/ml gabapentin.  
   
   
       16 . The process of  claim 15 , wherein the injectable pharmaceutical composition comprises about 80 mg/ml gabapentin.  
   
   
       17 . The process of  claim 1 , wherein the injectable pharmaceutical composition comprises between about 10 mg/ml and about 50 mg/ml gabapentin.  
   
   
       18 . The process of  claim 1 , wherein the injectable pharmaceutical composition comprises between about 20 mg/ml and about 40 mg/ml gabapentin.  
   
   
       19 . The process of  claim 1 , wherein the injectable pharmaceutical composition comprises about 30 mg/gabapentin.  
   
   
       20 . The process of  claim 1 , further comprising filtering the injectable composition.  
   
   
       21 . The process of  claim 20 , further comprising aseptically placing the filtered composition in a container to produce a container housing the filtered composition.  
   
   
       22 . The process of  claim 21 , wherein the heating comprises heating the container housing the composition.  
   
   
       23 . The process of  claim 1 , further comprising adjusting the pH of the injectable composition.  
   
   
       24 . The process according to  claim 23 , wherein the pH is adjusted by adding sodium hydroxide, hydrochloric acid, or both to the injectable composition.  
   
   
       25 . The process of  claim 1 , wherein the heating comprises autoclaving.