Pharmacokinetic behaviour of albendazole sulphoxide enantiomers in male and female sheep

Carles Cristòfol Adell, Maria Gloria Castells Carles, F Perez, Margarita Arboix Arzo, BPS Capece

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31 Citations (Scopus)

Abstract

Benzimidazole anthelmintic drugs are widely used in veterinary practice. Albendazole sulphoxide (ABZSO) is a benzimidazole drug with two enantiomers, as 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 T(max) 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.
Original languageEnglish
Pages (from-to)339-348
Number of pages9
JournalVeterinary Research Communications
Volume24
DOIs
Publication statusPublished - 20 Jun 2000

Keywords

  • Anthelmintic
  • Benzimidazole
  • Chromatography
  • Enantiomer
  • Metabolism
  • Pharmacokinet ics
  • Sex
  • Sheep

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