Time dependent pharmacokinetics of albendazole in human

Abstract The pharmacokinetics of the main metabolites of albendazole (albendazole sulphoxide (ABZ‐SO) and albendazole sulphone (ABZ‐SO2)) were studied in 12 healthy human volunteers in a double blind design on the first and last days of oral administration of 800 mg albendazole daily for 15 days. No significant differences were observed in Cmax, Tmax and Vd/F of ABZ‐SO, whereas the AUC, AUMC and T1/2 of this metabolite were significantly reduced and Cl/F was significantly increased in multiple dosing. There were also no significant differences in the Cmax, Tmax, Vd/F and T1/2 of ABZ‐SO2, whereas the AUC and AUMC of this metabolite were significantly reduced and Cl/F was significantly increased in multiple dosing. These observations suggest time dependent pharmacokinetics of albendazole (observed for ABZ‐SO and ABZ‐SO2), which was explained on the basis of the induction of enzymes involved in the metabolism of ABZ‐SO (albendazole sulphoxide) to metabolites other than albendazole sulphone in multiple dosing. Copyright © 2003 John Wiley & Sons, Ltd.