【摘要】 作者旨在研究替米考星明胶微球在兔体内的靶向性。采用高效液相色谱法测定肌内注射给药不同时间兔体各脏器组织的药物浓度,利用3p97药动学软件无房室模型计算药时曲线下面积,结果显示替米考星明胶微球肺脏的靶向效率较心脏、肌肉、肝脏和肾脏提高了5.18±0.13、3.11±0.06、3.94±0.06和3.74±0.02倍;肺脏、心脏、肌肉、肝脏和肾脏的相对摄取率分别为8.23±0.04、1.59±0.03、2.65±0.04、2.09±0.02和2.20±0.01;肺脏、心脏、肌肉、肝脏和肾脏的峰浓度比分别为2.22±0.04、0.42±0.02、0.46±0.01、0.61±0.02和0.71±0.02。表明替米考星明胶微球具有良好的肺靶向性,同时可以减轻替米考星的心脏毒性。更多还原

【Abstract】 The purpose of this study was to evaluate tilmicosin gelatine microsphere targeting.The timed tilmicosin concentrations of organs from tilmicosin gelatine microsphere and injection administered rabbits were detected with high performance liquid chromatography,and the area under curve was calculated with no compartment model by 3p97,a software of pharmacokinetics.Targeting parameters of tilmicosin gelatine microsphere were analysed.Compared with tilmicosin injection,lung targeting efficiency to heart′s,muscle′s,liver′s and kidney′s was elevated by 5.18±0.13,3.11±0.06,3.94±0.06,3.74±0.02 times,respectively.Relative intake rate of lung,heart,muscle,liver and kidney was 8.23±0.04,1.59±0.03,2.65±0.04,2.09±0.02 and 2.20±0.01.The ratio of peak concentration of lung,heart,muscle,liver and kidney was 2.22±0.04,0.42±0.02,0.46±0.01,0.61±0.02 and 0.71±0.02,respectively.It was concluded that tilmicosin gelatine microsphere had better lung targeting and alleviated the tilmicosin-induced cardiotoxicity.更多还原