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Pharmacokinetics of Tildipirosin in Ewes after Intravenous, Intramuscular and Subcutaneous Administration.
Animals ( IF 2.7 ) Pub Date : 2020-08-01 , DOI: 10.3390/ani10081332
Juan Sebastián Galecio 1, 2 , Elisa Escudero 1 , José Joaquín Cerón 3 , Giuseppe Crescenzo 4 , Pedro Marín 1
Affiliation  

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:

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。
更新日期:2020-08-01
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