Ricobendazole kinetics and availability following subcutaneous administration of a novel injectable formulation to calves

Res Vet Sci. 1998 Jul-Aug;65(1):5-10. doi: 10.1016/s0034-5288(98)90019-4.

Abstract

The plasma and abomasal fluid disposition kinetics of ricobendazole (RBZ) after subcutaneous (s.c.) administration of a novel injectable formulation to calves, and the comparative plasma availability after s.c. injection of RBZ and that obtained after oral treatment with albendazole (ABZ), were characterised. Six parasite-free Holstein calves received RBZ (solution 150 mg ml(-1)) by s.c. injection at 3.75 mg kg(-1) (Experiment 1). Experiment 2 was conducted in two experimental phases; in phase I, five calves (Group A) received RBZ by s.c. injection and five animals (Group B) were orally treated with ABZ (suspension 100 mg ml(-1)), at 5 mg kg(-1). Drug treatments were reversed for each group in phase II and given at 7.5 mg kg(-1). Samples of abomasal fluid (via cannula) and jugular blood were collected over 72 hours post-treatment and analysed by HPLC. RBZ and its sulphone metabolite were detected in plasma following its s.c. administration. RBZ was rapidly absorbed, reaching the plasma Cmax at 4.5 hours post-dosing. The sulphone metabolite followed a similar kinetic pattern. Both molecules were rapidly and extensively distributed into the abomasum, being detected in abomasal fluid between 30 minutes and 36 hours post-administration. An extensive plasma/abomasum exchange process, with ionic-trapping in the abomasum, accounted for the higher AUC value (>200 per cent) obtained for RBZ in abomasum compared with plasma. The s.c. treatment with RBZ formulated as a solution resulted in a significantly greater plasma availability (measured as ABZ sulphoxide) than the oral treatment with ABZ (suspension) given at the same dose rates.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Oral
  • Albendazole / administration & dosage
  • Albendazole / analogs & derivatives*
  • Albendazole / metabolism
  • Albendazole / pharmacokinetics*
  • Animals
  • Anthelmintics / administration & dosage
  • Anthelmintics / metabolism
  • Anthelmintics / pharmacokinetics*
  • Area Under Curve
  • Biological Availability
  • Cattle / blood
  • Cattle / metabolism*
  • Chromatography, High Pressure Liquid
  • Half-Life
  • Injections, Subcutaneous

Substances

  • Anthelmintics
  • Albendazole
  • albendazole sulfoxide