Pharmacokinetic Behaviour of Albendazole Sulphoxide Enantiomers in Male and Female Sheep |
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Authors: | Capece B.P.S. Castells G. Pérez F. Arboix M. Cristòfol C. |
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Affiliation: | (1) Departament de Farmacologia i de Terapèutica, Facultat de Veterinària, UAB 08193 Bellaterra, Spain |
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Abstract: | Benzimidazole anthelmintic drugs are widely used in veterinary practice. Albendazole sulphoxide (ABZSO) is a benzimidazole drug with two enantiomers, as a consequence of a chiral centre in the sulphoxide group. The kinetics of these enantiomers were studied in male and female sheep. Plasma samples were obtained from the animals between 0.5 and 72 h after oral administration of 7.5 mg/kg of a racemic formulation of ABZSO (total-ABZSO). After a liquid–liquid extraction, the samples were analysed by HPLC to determine the concentrations of total-ABZSO and of the sulphone metabolite (ABZSO2). During the chromatographic analysis, the ABZSO peak was collected and reanalysed by an HPLC technique using a Chiral AGP column to quantify the enantiomeric proportion therein. After kinetic analysis, the AUCs obtained for the (+)-ABZSO were 5.8 and 4.0 times higher than those for the (–)-ABZSO in male and female animals, respectively. The mean residence times were 23.4 and 16.1 h for (+)-ABZSO and 22.2 and 17.4 h for (–)-ABZSO for male and female animals, respectively. The only significant difference between the sexes (p<0.05) was in the Tmax of the (–)-ABZSO. Comparing both enantiomers within each sex, significant differences were found in all the kinetic parameters. Finally, no kinetic differences were found between sex for total-ABZSO or ABZSO2. |
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Keywords: | anthelmintic benzimidazole chromatography enantiomer metabolism pharmacokinetics sex sheep |
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