Abstract
1. The metabolic fate of [14C]fenclozic acid (ICI 54450) in rat was determined after intraduodenal administration at different doses.
2. Increasing the dose from 2 to 100mg/kg resulted in a five-fold increase in drug-related material secreted in bile.
3. At a dose of 2 mg/kg the taurine conjugate was a relatively minor metabolite, whereas at 100mg/kg this conjugate was the major metabolite in bile and urine.
4. Enhanced biliary secretion of the taurine conjugate in rats receiving multiple doses of fenclozic acid results in exposure of the intestinal cells to much greater concn. of drug-related metabolites.