[Absorption, distribution, metabolism and excretion of bacmecillinam. IV. Metabolites of bacmecillinam in human urine].

Bacmecillinam (KW-1100) metabolites and their excretion in human urine were investigated in the 3 male volunteers. After administration of KW-1100 capsules containing 80 mg (2 X 40 mg) as mecillinam to men, the urine samples up to 8 hours were collected for every 2 hours and analysed by high performance liquid chromatography and gas chromatography. The major metabolites in the human urine were mecillinam and 6-beta-[(hexahydro-1H-azepin-1-yl)-methyleneamino]-penicilloic acid (M-6), and minor quantities of M-4 and M-1 were also detected as the metabolites. Total recoveries of administered dose for the 3 volunteers were approximately 62, 81 and 73%, respectively. And M-1 excretion rate was lower than that in the case of rats and dogs. Hexamethyleneimine (HMI) as metabolite from the side chain was detected.