Pharmacokinetics of triclabendazole in rabbits |
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| Institution: | 1. Pharmaceutical Chemistry Department, Faculty of Pharmaceutical Sciences & Pharmaceutical Industries, Future University in Egypt, Cairo, Egypt;2. Analytical Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, Egypt;1. Laboratory of Toxicant and Drug Analysis, Federal University of Alfenas – UNIFAL-MG, Alfenas, MG, Brazil;2. Laboratory of Genetics and Molecular Cardiology, Heart Institute (InCor), Medical School, University of São Paulo, São Paulo, SP, Brazil;3. Department of Pharmacology, Universidade Federal de São Paulo (EPM-Unifesp), São Paulo, SP, Brazil;1. Medical Biochemistry Department, Faculty of Medicine, Zagazig University, Zagazig, Egypt;2. Clinical Oncology and Nuclear Medicine Department, Faculty of Medicine, Zagazig University, Zagazig, Egypt;3. Pathology Department, Faculty of Medicine, Zagazig University, Zagazig, Egypt;4. Surgery Department, Faculty of Medicine, Zagazig University, Zagazig, Egypt |
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| Abstract: | 1.Pharmacokinetic profiles of triclabendazole (TCBZ) following intravenous (i.v.) and oral administration of the drug in rabbits were carried out.2. In normal rabbits, TCBZ was metabolized rapidly to its sulphoxide (TCBZ-SO) and sulphone (TCBZ-SO2) derivatives following administration, with undetectable concentrations of unchanged TCBZ in the plasma 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 μg/ml and 9.5 μg/ml occurred 7.5 and 9.5 hr after oral administration, respectively.5. Both metabolites were eliminated slowly from plasma with elimination half-lives of 16.86 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 the sulphoxide, higher than that found for the sulphone, 185 g hr/l. |
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