Pharmacokinetics and Metabolism of Toltrazuil and Its Major Metabolites after Oral Administration in Broilers

  • Kim Myoung-Seok
    Jeollanamdo Development Institute for Traditional Korean Medicine, Jangheung, South Korea
  • Park Byung-Kwon
    Laboratory of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Chungnam National University, South Korea
  • Hwang Youn-Hwan
    Laboratory of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Chungnam National University, South Korea
  • Song In-Bae
    Laboratory of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Chungnam National University, South Korea
  • Kim Tea-Won
    Laboratory of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Chungnam National University, South Korea
  • Cho Jung-Hee
    Jeollanamdo Development Institute for Traditional Korean Medicine, Jangheung, South Korea
  • Ham Sung-Ho
    Jeollanamdo Development Institute for Traditional Korean Medicine, Jangheung, South Korea
  • Lim Jong-Hwan
    Center for Nutraceutical and Pharmaceutical Materials, Myoung Ji University, South Korea
  • Yun Hyo-In
    Laboratory of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Chungnam National University, South Korea

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抄録

Toltrazuril is a symmetrical tiazinetrione compound. It is active against all intracellular developmental stages including those of schizogony and gametogony. In this study the disposition kinetics of toltrazuril (TZR) and its major metabolites (TZR-SO and TZR-SO2) in broiler chickens after single oral administrations of 10 or 20 mg/kg were investigated. Mean plasma concentrations of TZR peaked at 16.4 and 25.2 μg/mL at 5.0 and 4.7 h after dosing, respectively. TZR was converted to the short-lived intermediary metabolite toltrazuril sulfoxide (TZR-SO), and then further metabolized to the reactive toltrazuril sulfone (TZR-SO2) being actually more slow eliminated with 80.3 and 82.9 h than TZR (10.6 and 10.7 h) or TZR-SO (14.8 and 15.3 h) in low and high dosing groups, respectively. Prolonged elimination half-life of TZR-SO2 could be interpreted as the persistent clinical efficacy of TZR in the treatment of protozoal parasites infection.

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