Abstract
Repaglinide is a short‐acting antidiabetic drug. It is used in type II diabetic patients to normalize postprandial hyperglycemia. Metabolism and excretion of [ 14 C]‐repaglinide in healthy male volunteers were investigated following multiple oral dosing of 2 mg. Five oxidative metabolites were identified, including an aromatic amine ( 2 ) and a dicarboxylic acid ( 3 ), both formed by the opening of the piperidine ring; metabolites yielded by hydroxylation of the piperidine ring, O‐deethylation, and hydroxylation on the isopropyl moiety. Phase II metabolites of acylglucuronide conjugate and tauride conjugate were also detected. The parent compound accounted for 61% of the total radioactivity in plasma, followed by the major metabolite 3 (11%), which was also the major metabolite in feces. Metabolites 2 (24%) and 3 (22%) were the major urinary metabolites.
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