急性实验性家兔肝肾损害对依诺沙星药代动力学影响的研究

Pharmacokinetic Effect on Enoxacin in Acute Experimental Liver and Renal Injuries

建立了测定兔血清中依诺沙里的高效液相色谱仪检测法，方法平均回收率为92.9％，最低检出浓度为1.7μg。研究了急性实验性肝肾损伤家兔（各5只）口服1次依诺沙星后的药代动力学。其血药浓度-时间数据用二室模型拟会，肝损伤组消除相指数、消除相半衰期、消除速率常数及清除率4个药代动力学参数与对照组相比差异无显著意义;肾损伤组4个参数与对照组相比有显著差异。结果显示肾损伤组对依诺沙星的清除率明显减慢，故肾损伤时有必要减少用药剂量及给药次数。

HPLC assay for the determination of enoxacin in rabbit serum was established. The mean recovery of method was 92. 9 % and minimum detective concentration was 1. 7 μg. The pharmacokinetics of enoxacin was studied after a single oral dose of enoxacin in five acute experimental liver injuries and five acute experimental renal injuries of rabbits. The serum concentration-time profiles conformed to a two-compartment open model. There was no significant difference between liver injuries and the control group for the four parameters: β,t1/2β,K10 as well as CLs. This suggests that liver injuries had little innuence on the pharmacokinetics of enoxacin. Significant difference was found between renal injuries and the control group for the four parameters. Since the clearance of enoxacin was lowered significantly in renal injuries, the dosage and intervals of drugs to be taken must be redesigned.