Formulations of canfosfamide and their preparation

Abstract

Formulations of canfosfamide and their preparation.

1 . A formulation of canfosfamide consisting essentially of (50±5) mg/mL canfosfamide hydrochloride in (100±10) mM aqueous sodium citrate buffer at pH 4.6±0.2. 
   
   
       2 . The formulation of  claim 1  consisting essentially of 50 mg/mL canfosfamide hydrochloride, 100 mM sodium citrate dihydrate, and 2.9 mM citric acid monohydrate in water, at pH 4.6±0.2. 
   
   
       3 . A method of preparing the formulation of  claim 1 , comprising:
 (a) preparing a sodium citrate buffer at pH 6.5±0.1,   (b) dissolving the canfosfamide hydrochloride in the buffer, and   (c) if necessary, adjusting the pH of the resulting solution to pH 4.6±0.2.   
   
   
       4 . The method of  claim 3  where the buffer is prepared using less than the volume of water needed to achieve the final concentrations of the formulation, and the method further comprises:
 (d) adding water to achieve the final concentrations.   
   
   
       5 . The method of  claim 4  where the buffer is prepared by dissolving solid sodium citrate and then citric acid in water, and the volume of water into which the sodium citrate is dissolved is (85-95)% of the volume of water needed to achieve the final concentrations of the formulation. 
   
   
       6 . The formulation that is the product of the method of  claim 3 . 
   
   
       7 . A lyophilized formulation consisting essentially of the lyophilization product of the formulation of  claim 1 .