Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats

• Published in: The veterinary journal (1997) Vol. 177; no. 2; pp. 297 - 299
• Main Authors: Capece, Bettencourt P.S., Castells, Gloria, Godoy, Carlo, Arboix, Margarita, Cristòfol, Carles
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01-08-2008
• Subjects: Administration, Oral; albendazole; Albendazole - administration & dosage; Albendazole - analogs & derivatives; Albendazole - blood; Albendazole - chemistry; Albendazole - pharmacokinetics; Albendazole sulfoxide; animal diseases; animal models; Animals; Anthelmintics - administration & dosage; Anthelmintics - blood; Anthelmintics - chemistry; Anthelmintics - pharmacokinetics; dosage; Dose-Response Relationship, Drug; drug evaluation; drug formulations; drug therapy; Enantiomers; Enantioselectivity; helminthiasis; Isomerism; metabolites; oral administration; Pharmacokinetics; Rats; veterinary drugs; veterinary medicine; Rats; Enantioselectivity; Enantiomers; Pharmacokinetics; Albendazole sulfoxide
• ISSN: 1090-0233; 1532-2971
• DOI: 10.1016/j.tvjl.2007.04.011

The pharmacokinetic behaviour of albendazole sulfoxide (ABZSO) enantiomers was studied in rats after the oral administration of 10
mg/kg of
rac-ABZSO, 5
mg/kg of (−)-ABZSO or 5
mg/kg of (+)-ABZSO. The disposition profiles of ABZSO enantiomers were similar in all treatments, but the calculated area under the curve for the (−)-ABZSO was higher in all cases compared with (+)-ABZSO. The results suggest that there is no chiral inversion of ABZSO enantiomers. After the administration of
rac-ABZSO, 17.2% of the total dose was recovered in urine as albendazole ABZ (0.1%), albendazole sulfone ABZSO
2 (0.3%), albendazole 2-aminosulfone (ABZ-SO
2NH
2) (3.1%) and ABZSO (13.7%). The ratio (+) to (−) was similar in urine (1.6) and blood (1.7).