Aripiprazole complex formulation and method

Abstract

An aripiprazole formulation is provided which includes the antipsychotic agent aripiprazole in the form of an inclusion complex in a β-cyclodextrin, preferably, sulfobutyl ether β-cyclodextrin (SBECD), which in the form of an injectable produces reversible generally minimal to mild irritation at the intramuscular injection site. A method for minimizing or reducing irritation caused by aripiprazole at an intramuscular injection site and a method for treating schizophrenia employing the above formulation are also provided.

1 . An aqueous injectable formulation having a pH of from about 3.5 to about 5, comprising:
 a) a complex comprising aripiprazole and sulfobutyl ether-β-cyclodextrin;   b) tartaric acid;   c) sodium hydroxide; and   d) water for injection.   
     
     
         2 . The formulation as defined in  claim 1  which contains 2 mg aripiprazole/ml, 5 mg aripiprazole/ml or 7.5 mg aripiprazole/ml. 
     
     
         3 . The formulation as defined in  claim 1  having a pH of about 4.3. 
     
     
         4 . The formulation as defined in  claim 1  comprising from about 0.1 to about 2.5% by weight aripiprazole. 
     
     
         5 . The formulation as defined in  claim 1  comprising from about 0.2 to about 1.5% by weight aripiprazole. 
     
     
         6 . The formulation as defined in  claim 1  wherein the sulfobutyl ether-β-cyclodextrin is present in an amount from about 100 to about 700 mg/ml of solution. 
     
     
         7 . The formulation as defined in  claim 1  wherein the tartaric acid is present in an amount from about 7 to about 9 mg/ml. 
     
     
         8 . The formulation as defined in  claim 1  wherein the tartaric acid and the sodium hydroxide are present in amounts to impart a pH of about 4.3 to the formulation.