[Human pharmacokinetics and metabolism of 14C-labeled gliquidone (AR-DF 26)]

Investigations of pharmacokinetics and metabolism of 14C-labelled 1-cyclohexyl-3 (p-[2-(3,4-dihydro-7-methoxy-4,4-dimethyl-1,3-dioxo-2-(1H)-isoquinolyl)-ethyl]-phenyl)-sulfonyl)-urea (AR-DF 26; gliquidone; Glurenorm) after i.v. and oral applications were carried out on 10 healthy volunteers. After oral application of 15 mg AR-DF 26, maximum blood levels of 370 ng/ml blood or 700 ng/ml plasma, respectively, were reached. After i.v. as well as oral application of AR-DF 26 in men the bulk of the substance applied was excreted with the faeces and only 5 percent were found in urine. After both modes of application the metabolites in the faeces were found to be quantitatively and qualitatively similar. The structure of 4 metabilites was demonstrated by isotope dilution analysis.