Metabolic disposition of ivermectin in tissues of cattle, sheep, and rats.

作者: B. H. Arison , E. Sestokas , R. Sestokas , Shuet-Hing Lee Chiu , R. P. Buhs

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摘要: The metabolic disposition of ivermectin, a new antiparasitic drug, has been studied in cattle, sheep, and also rats dosed with the drug labeled tritium C-22,23 positions. In edible tissues these animals, unaltered was major tissue residue component quantitated by HPLC-reverse isotope dilution assay. depletion half-lives ranged between 1 6 days, similar to those total species. Most metabolites present liver were more polar than parent drug. Based on spectral (NMR, mass spectrometric) analysis chromatographic comparison authentic compounds prepared vitro rat or steer microsomal incubations, three have isolated identified as hydroxylation derivatives i.e. 24-hydroxymethyl-H2B1a, its monosaccharide, 24-hydroxymethyl-H2B1b.

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