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Chirality of the sulphoxide metabolites of fenbendazole and albendazole in sheep
Authors:P. DELATOUR  E. BENOIT  F. GARNIER  S. BESSE
Affiliation:Department of Biochemistry, National School of Veterinary Medicine of Lyon, France.
Abstract:Two prochiral sulphide drugs, fenbendazole (FBZ) and albendazole (ABZ) were administered orally to sheep. Blood samples were analysed for parent drug and S-oxidation metabolites and the chirality of the sulphoxide metabolites was determined. The plasma concentrations of the enantiomers of the sulphoxides were never a racemate. On the contrary, the ratios were greater than 1 as soon as the sulphoxide compounds could be detected in plasma. They subsequently increased linearly throughout the time course of the kinetics, reaching the level 86:14 after FBZ and 95:5 after ABZ treatment. The major enantiomer represented 74% and 86% of the total AUC of SO.FBZ and SO.ABZ, respectively.
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