PHARMACOKINETICS OF TRICLABENDAZOLE IN RABBITS

1. Pharmacokinetic profiles of triclabendazole (TCBZ) following intrav enous (i.v.) and oral administration of the drug in rabbits were carri ed out. 2. In normal rabbits, TCBZ was metabolized rapidly to its sulp hoxide (TCBZ-SO) and sulphone (TCBZ-SO2) derivatives following adminis tration, with undetectable concentrations of unchanged TCBZ in the pla sma of the treated animals at any time (detection limit, 10 ng/ml). 3. The disposition kinetics of this drug in rabbits can be described by a two-compartment open model. 4. Mean peak concentrations in plasma of TCBZ-SO and TCBZ-SO2 of 12.41 mu g/ml and 9.5 mu g/ml occurred 7.5 an d 9.5 hr after oral administration, respectively. 5. Both metabolites were eliminated slowly from plasma with elimination half-lives of 16.8 6 hr for the sulphoxide and 13 hr for the sulphone. 6. The area under the plasma concentration versus time curve (AUC) was 240 mg hr/l for t he sulphoxide, higher than that found for the sulphone, 185g hr/l.