Time dependent pharmacokinetics of albendazole in human.
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.
Mirfazaelian
A
A
Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, PO Box 14155/6451, Tehran, Iran.
Rouini
M R
MR
Dadashzadeh
S
S
D000284:Administration, Oral; D000328:Adult; D015766:Albendazole / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000378:metabolism / Q000493:pharmacokinetics*; D000871:Anthelmintics / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D019540:Area Under Curve; D004311:Double-Blind Method; D004334:Drug Administration Schedule; D005260:Female; D006207:Half-Life; D006801:Humans; D008099:Liver / Q000378:metabolism; D008297:Male; D013997:Time Factors
D000871:Anthelmintics; C027187:albendazole sulfone; D015766:Albendazole; C027186:albendazole sulfoxide