Rapid and Sensitive Characterization of the Metabolite Formation Enzyme Kinetics of Radiolabeled Drugs Using Stop-Flow Liquid Radiochromatography

This study evaluated the reproducibility, sensitivity, accuracy, and precision of stop-flow liquid radiochromatographic detection (RFD). Stop-flow RFD was about 10-fold more sensitive compared with traditional RFD and had a good reproducibility for quantification and HPLC retention time. Stop-flow RFD was applied to determine enzyme kinetics of radiolabeled drugs. The enzyme kinetic parameters of muraglitazar glucuronidation determined by stop-flow RFD were comparable with those determined by microplate scintillation counting (MSC).