HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHIC DETERMINATION OF CILASTATIN AND ITS MAJOR METABOLITE N-ACETYLCILASTATIN IN RAT PLASMA, URINE AND BILE

A new high-performance liquid chromatographic method coupled with solid-phase (C-8) sample extraction has been developed for the simultaneous quantification of cilastatin and its major metabolite N-acetylcilastatin in rat plasma, urine and bile. The method is linear, reproducible and reliable with a detection limit of 1-mu-g/ml in all three fluids. Plasma concentrations of cilastatin and N-acetylcilastatin at selected time intervals and biliary and urinary recoveries of cilastatin and N-acetylcilastatin following an intravenous dose of 10 mg/kg cilastatin are presented.