A single-dose disposition kinetics for tildipirosin was evaluated in clinically healthy ewes (n = 6) after intravenous (IV), intramuscular (IM), and subcutaneous (SC) administration of a commercial formulation. Tildipirosin concentrations were determined by high-performance liquid chromatography with ultraviolet detection. Plasma concentration-time data was calculated by non-compartmental pharmacokinetic methods. The apparent volume of distribution (Vz) of tildipirosin after IV administration was 5.36 ± 0.57 L/kg suggesting a wide distribution in tissues and inside the cells. The elimination half-life (t½λz) was 17.16 ± 2.25, 23.90 ± 6.99 and 43.19 ± 5.17 h after IV, IM and SC administration, respectively. Following IM administration, tildipirosin was rapidly absorbed (tmax = 0.62 ± 0.10 h) even to a greater extent than after SC administration. Time to reach peak concentration (tmax) and peak plasma concentrations (Cmax) differed significantly, but both parameters showed a more significant variability after SC than after IM administration. Bioavailabilities after extravascular administration were high (>70%). Therefore, given general adverse reactions that were not observed in any ewe and favourable pharmacokinetics, tildipirosin could be effective in treating bacterial infections in sheep.

中文翻译：

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静脉，肌肉内和皮下给药后，Tildipirosin在母羊中的药代动力学。

对于tildipirosin单剂量处置动力学在临床上健康的母羊进行评价（Ñ= 6）在静脉内（IV），肌内（IM）和皮下（SC）施用市售制剂后。高效液相色谱法和紫外线检测法测定提尔吡罗辛的浓度。通过非房室药代动力学方法计算血浆浓度-时间数据。静脉给药后，替地吡辛的表观分布体积（Vz）为5.36±0.57 L / kg，表明在组织内和细胞内部分布广泛。IV，IM和SC给药后，消除半衰期（t1 /2λz）分别为17.16±2.25、23.90±6.99和43.19±5.17 h。IM给药后，tildipirosin被迅速吸收（tmax = 0.62±0.10 h），甚至比SC给药后更大。达到峰值浓度（tmax）的时间和峰值血浆浓度（Cmax）的时间显着不同，但是SC后两个参数均比IM给药后显示出更大的变异性。血管外给药后的生物利用度很高（> 70％）。因此，鉴于在任何母羊中都未观察到的一般不良反应和良好的药代动力学，替地吡辛可有效治疗绵羊的细菌感染。