[Hydroxylation of glibenclamide by liver biopsy specimens]

A method for measuring hydroxylation rates of the oral antidiabetic agent glibenclamide (Euglucon) by liver biopsy specimens is described. After incubation of the material in a buffer system, containing glibenclamide-14-C, the supernatant is extracted with organic solvent. The extract is condensed and the radioactivity of the spots after thin-layer chromatography is measured. A linear relationship between incubation time and hydroxylation rates could be demonstrated. Equal amounts of the two metabolites, 4-trans- and 3-cis-hydroxy-cyclohexyl-glibenclamide were formed.