Comparative disposition of ricobendazole enantiomers after intravenous and subcutaneous administration of a racemic formulation to calves

Carles Cristfol, Guillermo Virkel, Luis Lvarez, Margarida Arboix, Carlos E. Lanusse

Research output: Contribution to journalArticleResearchpeer-review

18 Citations (Scopus)

Abstract

The enantioselective disposition kinetics of the benzimidazole anthelmintic, ricobendazole (RBZ), have been characterized after its intravenous (iv) and subcutaneous (sc) administration as a racemic formulation to cattle. The (+) and (-) RBZ enantiomeric forms were recovered in plasma after iv and sc administration of the racemic RBZ formulation, using a chiral phase based HPLC method. A biexponential plasma concentration versus time curve was observed for both RBZ enantiomers following the iv treatment. Total body clearance was higher for (-) RBZ (150.4 mL/h · kg) compared with that obtained for the (+) RBZ antipode (78.1 mL/h · kg). The elimination half-life of the (-) RBZ enantiomer was shorter (T1/2β: 2.67 h) compared with the (+) enantiomer (T1/2β: 5.41 h). The plasma availability (expressed as AUC) was significantly higher for (+) RBZ compared with that obtained for the (-) antipode following both treatments. The enantiomeric ratio in plasma at To was close to unity (50% of each enantiomer); the analysis of the concentration ratios (+) RBZ/(-) RBZ, demonstrated an increase in the proportion of (+) RBZ during the time course of the kinetics after both iv and sc treatments. The results presented herein show the enantioselective disposition kinetics of RBZ in cattle and are a further contribution to the understanding of the kinetic behaviour of these sulphoxide-containing benzimidazole anthelmintics in ruminants. Copyright © 2000 John Wiley & Sons, Ltd.
Original languageEnglish
Pages (from-to)303-311
JournalBiopharmaceutics and Drug Disposition
Volume21
DOIs
Publication statusPublished - 1 Dec 2000

Keywords

  • Benzimidazole
  • Calves
  • Distribution
  • Enantiomers
  • Kinetics

Fingerprint Dive into the research topics of 'Comparative disposition of ricobendazole enantiomers after intravenous and subcutaneous administration of a racemic formulation to calves'. Together they form a unique fingerprint.

Cite this