Rapid in vitro and in vivo conversion of hydroxymethyl-nitrofurantoin into nitrofurantoin as measured by HPLC

Abstract

For the first time a method of separation between nitrofurantion and hydroxymethylnitrofurantoin is reported. Until now it has not been possible to separate these two substances because of a rapid degradation of hydroxymethyl-nitrofurantoin into nitrofurantion in, for instance, dimethylformamide and aqueous non-acid solutions.

In vivo studies after administration of a commercially available formulation containing hydroxymethyl-nitrofurantoin, showed only nitrofurantoin to be present in urine. This formulation itself was also partly degraded. These results show that hydroxymethylnitrofurantoin acts as a pro-drug of nitrofurantoin.