【摘要】 目的 :研究中国内江猪肾脏排泄的药代动力学特点及头孢唑啉 (CEZ)血浆蛋白结合率。方法 :选择主要经肾脏排泄的CEZ为模型药 ,采用高效毛细管电泳法测定其血药浓度 ,并计算药代动力学参数 ;采用平衡透析法测定其血浆蛋白结合率。结果 :中国内江猪静注CEZ后 ,其代谢符合二室开放模型。血浆清除率 (Cls)为 8 3 5ml/kg·min 1,消除半衰期 (t1/ 2 β)为 2 7 3 5min。中国内江猪血浆白蛋白浓度为 45 5 4± 1 7 44μmol·L 1,CEZ蛋白结合率为 80 5 9%～ 5 8 2 2 % ,解离常数为 1 6 1 0± 2 67μmol·L 1。结论 :与正常人实验药动学参考值相比较 ,内江猪对CEZ的消除与人具有相似的规律 ,但清除率明显大于人。侧面提示肾脏排泄功能可能较人强。内江猪血浆白蛋白浓度、CEZ蛋白结合率较人低 ,而解离常数较人高 ,表明CEZ与中国内江猪血浆蛋白结合的动态平衡中 ,结合物稳定性差 ,处于游离状态的CEZ较多 ,更易于消除更多还原

【Abstract】 Objective: The study was to investigate the kidney cekazoline elimination of neijiang pig. Methods: The serum concentration of cefazolin and plasma protein binding rate in neijiang pig was detected by high performance capillary electrophoresis. Results: The pharmacokinetic parameters of CEZ were calculated as two compartment model in neijiang pig. The clearance of CEZ was 8.35±0.019ml/kg/min; the half life time of elimination was 27.35±6.32 min in neijiang pig. The albumin concentration were 455.4±17.44μmol/l, CEZ plasma protein binding rate were 80.59～58.22%, dissociation constant were 16.10±2.67μmol/l. Conclusions: The above results compared with Chinese normal human pharmacokinetic parameters, indicated that the elimination of CEZ in neijiang pig was quicker than that in human. The albumin and CEZ plasma protein binding rate in neijiang pig were less than that in human, there fore the amount of free CEZ were more higher than in human, which contributed to the elimination of CEZ.更多还原