国产碘醚柳胺在绵羊体内的药代动力学及组织残留量的研究

The Study on the Pharmacokinetics and Tissue Residues of Rafoxanide in Sheep

给绵羊单剂量口服碘醚柳胺(7.5mg/kg),用HPLC法测定不同时间的血浆药物浓度。结果,碘醚柳胺在血浆中药物代谢动力学符合开放性二室模型,动力学方程为: C_t=208.586 8e^(-0.4756(t-0.5426))+18.760 5e^(-0.0439(t-0.5426))-227.445e^(-0.5328(t-0.5426))口服碘醚柳胺后,达峰时间(Tmax)为3.698 9±0.197 4d;峰浓度(Cmax)为18.760 5±1.564 6μg/mL;消除半衰期(T(1/2)β)为15.800 6±0.445 7d;曲线下面积(Auc)为459.000 0±62.531 3μg·d/mL。碘醚柳胺在绵羊的肝、肾、胆汁、肌肉中的残留量:停药后28d分别为0.359 9、0.243 2、0.157 9、0.100 0μg/g;停药后50d,肝脏中的残留量为0.100 0μg/g,其它组织中均检测不到;停药后60d,各组织中均无残留。

The concentrations of rafoxanide in plasma and tissues of sheepwhich orally given rafoxanide as a capsule of a dose rate of 7.5 mg/kg bodyweight were determined by high-performance liquid chromatography (HPLC).The results showed that the pharmacokinetics of rafoxanide in normal sheepfitted a two-compartment open model with an equation: Ct = 208.586 8e^(-0.4756) (t-0.5426) + 18.760 5 e^(0.0439) (t-0.5426) - 227.445 e^(-0.5328)(t-0. 5426). The average area under curve (Auc) was 459.000 0±62.531 3mg·d/mL. The average elimination half-life was 15.800 6±0.445 7 days; andthe average peak concentration in sheep 18.760 5±1.564 6 μg/mL at 3.698 9±0.197 4 days after administration. The tissue residue of rafoxanide: 0.359 9,0.243 2, 0.157 9, 0.100 0 μg/g occurred in liver, kidney, bile and musclerespectively after 28 days of administration; 0.1μg/g in liver after 50 days;and no residue was detectable in any tissue at 60 days postdosing.