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Bioconversion of netobimin pro-drug by gastrointestinal fluids of ruminants

European Journal of Drug Metabolism and Pharmacokinetics volume 17, pages 121–128 (1992)Cite this article

Summary

The biotransformation of netobimin (NTB) pro-drug by ruminai, abomasal and intestinal fluids of sheep and cattle was investigated under anaerobic conditions in vitro. No metabolic conversion of NTB was observed upon incubation with abomasal fluid or boiled samples of different gastrointestinal fluids. NTB pro-drug was reduced and cyclised into albendazole (ABZ) and this further oxidized into ABZ sulphoxide (ABZSO) and ABZ sulphone (ABZSO2) by both sheep and cattle ruminai and ileal fluids. A zwitterion formulation of NTB produced a significantly greater amount of anmelminthically active ABZ metabolites (ABZ and ABZSO) than a trisamine salt formulation of the same compound. Although there was no difference in the total amount of products formed, both cattle ruminai and ileal fluids showed a greater oxidative capacity than sheep derived fluids. This was evidenced by the greater amounts of ABZSO recovered and by the resultant lower ratios of ABZ/ABZSO obtained with cattle fluids.

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Affiliations

  1. Institute of Parasitology of McGill University, Macdonald Campus 21, 111 Lakeshore Road, H9X1C0, Ste-Anne de Bellevue, Québec, Canada

    C. E. LANUSSE, B. NARE, L. H. GASCON & R. K. PRICHARD

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  1. C. E. LANUSSE
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  2. B. NARE
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  3. L. H. GASCON
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  4. R. K. PRICHARD
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LANUSSE, C.E., NARE, B., GASCON, L.H. et al. Bioconversion of netobimin pro-drug by gastrointestinal fluids of ruminants. Eur. J. Drug Metab. Pharmacokinet. 17, 121–128 (1992). https://doi.org/10.1007/BF03188780

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  • DOI: https://doi.org/10.1007/BF03188780

Keywords

  • Biovconversion
  • netobimin
  • albendazole
  • gastrointestinal fluids
  • sheep
  • cattle