【摘要】 对10例健康志愿者按50mg单剂量和多剂量口服依帕司他（Epalrestat）后的药代动力学进行了研究。多剂量给药方案按q8h共服药10次。应用高效液相色谱一紫外检测方法测定依帕司他血药浓度。血药浓度数据用3p87药代动力学软件处理，按两室模型拟合并求算药代动力学参数。单剂量给药后的药代动力学参数分别为：Tmax2.25±0．95h，Cmax4104.91±849．87·g·L-1，AUC13016．6±2865.4μg·h·L－1，T1/2β1.11±0.35h。多剂量给药达稳态后的药代动力学参数分别为：Tmax2．00±1.03h，Cmin146．24±54．50μg·L-1，Cmax4769．99±897.86μg·L-1，Cavg1789.03±416.04μg·L-1，AUC14689.5±3472.3μg·h·L-1，T1/2β1.21±0.26h。依帕司他在人体内的吸收速度和消除速度不随连续给药变化，按50mg，q8h方案给药，药物在体内基本没有蓄积，性别对药代动力学参数没有影响。更多还原

【Abstract】 The pharmacokinetics of epalrestat were investigated after single and multipleoral doses of 50mg of epalrestat in 10 healthy volunteers(male 5, female 5). Multiple-dose regimens used 8-hour dosing intervals for 10 doses. Plasma epalrestat concentrationswere measured using high-performance liquid chromatography. The concentration-timecurves of epalrestat were fitted to a two-compartment open model.The pharmacokineticparameters obtained from the single-dose study were as follows:Tmax2.25±0．95h，Cmax 4104.91±849．87·g·L-1，AUC 13016．6±2865.4μg·h·L－1，T1/2β1.11±0.35hThe steady-state pharmacokinetic parameters were:Tmax2．00±1.03 h， Cmin 146．24 ± 54．50μg·L-1， Cmax 4769．99 ± 897.86μg·L-1， Cavg1789.03±416.04μg·L-1，AUC 14689.5±3472.3μg·h·L-1，T1/2β1.21±0.26h。 The absorption rate and elimination rate ofepalrestat were not changed after multiple oral administration. There was no accumulationof drug in plasma to be found after the repeated administration with the 50mg, q.8hregimen and no difference in pharmacokinetics of epalrestat in male and female volunteerswas observed. Lender has no effect on its pharmacokinetics.更多还原