替米考星固体分散体在猪体内的药代动力学研究

Pharmacokinetics of Tilmicosin Solid Dispersion in Swines

研究替米考星固体分散体在猪体内的药代动力学特征,并评价其与市售替米考星肠溶颗粒的生物等效性。采用高效液相色谱法(HPLC)测定血浆中替米考星浓度,通过PKSolver 2.0药动学程序计算药动学参数。市售替米考星肠溶颗粒和替米考星固体分散体在猪体内的药动学行为均符合一级吸收一室模型,T_(max)分别为(2.72±0.14)、(2.55±0.21)h,C_(max)分别为(1.53±0.26)、(1.81±0.19)μg/mL,AUC_(0-∞)分别为(33.31±2.19)、(45.47±2.62)μg·h/mL,替米考星固体分散体相对肠溶颗粒的相对生物利用度提高至136.5%。结果表明,替米考星固体分散体具有更好的肠溶缓释作用及更高的生物利用度,具有一定的生物安全性,在猪体内保持药效时间更久。

Study the pharmacokinetics of tilmicosin solid dispersion in pigs and evaluate its bioequivalence with commercial tilmicosin enteric coated granules.The plasma concentrations of tilmicosin were analyzed by HPLC.The pharmacokinetic parameters were calculated by PKSolver 2.0 pharmacokinetic program.The concentration-time curve of tilmicosin solid dispersion and commercial tilmicosin enteric coated granules were fitted a two compartment open model with first order absorption.The main pharmacokinetic parameters of T_(max) were(2.72±0.14)(2.55±0.21)h,C_(max) were(1.53±0.26)(1.81±0.19)ug/ml,AUC_(0-∞)were(33.31±2.19)(45.47±2.62)ug·h/ml.The relative bioavailability of tilmicosin SD group was increased to 136.5%compared with enteric coated granule group.In conclusion,tilmicosin solid dispersion shows better performance of sustained release,which improves biosafety and last longer in pig.