Time dependent pharmacokinetics of albendazole in human.

Author(s): Mirfazaelian A, Rouini MR, Dadashzadeh S

Affiliation(s): Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, PO Box 14155/6451, Tehran, Iran.

Publication date & source: 2003-07, Biopharm Drug Dispos., 24(5):199-204.

Publication type: Clinical Trial; Randomized Controlled Trial

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 C(max), T(max) and V(d)/F of ABZ-SO, whereas the AUC, AUMC and T(1/2) of this metabolite were significantly reduced and Cl/F was significantly increased in multiple dosing. There were also no significant differences in the C(max), T(max), V(d)/F and T(1/2) 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.