舍曲林在中国健康志愿者体内的药代动力学研究

目的对中国健康志愿者口服不同剂量盐酸舍曲林片后进行药代动力学研究,探讨舍曲林在国人体内的药代动力学特征。方法12名中国健康男性志愿者按拉丁方设计分别口服3种单剂量盐酸舍曲林片(50、100、150 mg),用固相萃取结合高效液相色谱紫外检测法测定血浆中舍曲林的浓度,采用DAS软件拟合药代动力学参数和统计分析。结果计算所得的药动学参数显示,口服50、100、150 mg盐酸舍曲林片的AUC0-96分别为(437.51±80.78)、(804.19±178.11)和(1154.57±243.92)μg.h.L-1;Cm ax分别为:(11.70±2.40)、(22.84±7.05)和(32.61±7.95)μg.L-1,受试者血药浓度随单剂量给药量的增加呈比例的升高,不同剂量组的AUC0-t/Dose、Cm ax/Dose比值间差异无统计学意义(P>0.05)。结论盐酸舍曲林在中国人体内的过程(剂量范围为50~150 mg)显示线性药代动力学特征。

Study on pharmacokinetic of sertraline in chinese healthy volunteers

Aim To explore the pharmacokinetic characteristic of sertraline in Chinese healthy male volunteers.Methods The 12 healthy volunteers were divided into receiving orally a single dose of 50,100,150 mg sertraline tablets respectively,in latin square design study.After administration of sertraline tablets,the plasma concentration were determined using UV-HPLC with solid phase extraction method.The pharmacokinetics parameters were analyzed by DAS program.Results It was found that plasma levels increased after orally increased dosage of sertraline in the healthy volunteers exhibited a dose-dependent manner.The pharmacokinetic parameters calculated were the follows: AUC_(0-96) of three different dosages(50,100,150 mg) are(437.51±80.78),(804.19±178.11) and(1154.57±243.92) μg·h·L~(-1);and C_(max) are(11.70±2.40),(22.84±7.05) and(32.61±7.95) μg·L~(-1) respectively.There were no significant differences in AUC_(0-t)/dose,C_(max)/dose between the group(P>0.05).Conclusion The pharmacokinetic characteristic of sertraline in Chinese healthy volunteers(in 50~150mg process) were fitted with linear kinetic model.