Rapid and sensitive characterization of the metabolite formation enzyme kinetics of radiolabeled drugs using stop-flow liquid radiochromatography

Drug Metab Lett. 2008 Jan;2(1):41-6. doi: 10.2174/187231208783478470.

Abstract

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).

Publication types

  • Comparative Study
  • Validation Study

MeSH terms

  • Buspirone / metabolism
  • Carbon Radioisotopes
  • Chromatography, High Pressure Liquid / methods*
  • Chromatography, High Pressure Liquid / standards
  • Glucuronides / metabolism
  • Glycine / analogs & derivatives*
  • Glycine / metabolism
  • Humans
  • Indoles / metabolism
  • Microsomes, Liver / metabolism
  • Oxazoles / metabolism*
  • Reproducibility of Results
  • Scintillation Counting / methods

Substances

  • BMS204352
  • Carbon Radioisotopes
  • Glucuronides
  • Indoles
  • Oxazoles
  • Glycine
  • Buspirone
  • muraglitazar