High-performance liquid chromatographic comparison of in vivo and in vitro drug metabolism.

Using 2-ethyl-3-(4- hydroxybenzoyl )benzofuran ( EHBB ) as an example, biotransformation in rabbits and rats and by rat hepatocyte suspensions was studied by high-performance liquid chromatography (HPLC) and mass spectrometry. The biotransformation of N-alkyl-substituted piperidines by rat hepatocytes gives valuable information about the pharmacodynamics of this series of compounds. It is demonstrated that a simple reversed-phase HPLC pre-column technique is much superior to the classical sample purification via extraction. The utility of hepatocytes for the investigation of drug metabolism is demonstrated.