硫普罗宁片人体药动学及生物等效性研究.PDFVIP

硫普罗宁片人体药动学及生物等效性研究 王晓波1 1 1 2 3 3 3 ，袭荣刚 ，刘丹 ，程申强 ，谢小青 ，关屹 ，刘洋 (1.解放军大连第210 医院国家药物临床试验机构，辽宁 大连 116021 ；2.上海迪冉郸城制药有限公司，上海 200000 ；3.沈阳亿灵医药有限公司，沈阳 110179) 摘要：目的 研究健康受试者口服硫普罗宁片后的药动学及不同制剂间生物等效性。方法 LC-MS/MS 测定硫普罗宁受 试制剂和参比制剂给药后血浆中硫普罗宁的血浆药物浓度，用DAS 软件计算药动学参数，并比较两制剂在健康人体的生 物等效性。结果 硫普罗宁片受试制剂和参比制剂的主要药动学参数是：t1/2 分别为(12.8±5.3)和(10.8±4.6) min ；Cmax 分别 为(7.02±1.35) 和(7.16±0.81) g·mL1 ；AUC0-t 分别为(44.0±8.3) 和(45.5±6.5) g·h·mL1 ；AUC0-∞ 分别为(50.1±10.7) 和 (50.7±9.5) g·h·mL1。受试制剂与参比制剂相比，在人体的相对生物利用度为(96.8±11.5)% 。结论 硫普罗宁两种制剂药动 学参数没有显著性差异，具有生物等效性。 关键词：硫普罗宁；液相色谱-质谱法；药动学；生物等效性 中图分类号：R917.103 文献标志码：B 文章编号：1007-7693(2011)04-0368-05 Pharmacokinetics and Bioequivalence of Two Tiopronin Preparations in Healthy Volunteers 1 1 1 2 3 3 3 WANG Xiaobo , XI Ronggang , LIU Dan , CHENG Shenqiang , XIE Xiaoqing , GUAN Yi , LIU Yang (1.State Agencies of Drug Clinical Trials, The 21 0th Hospital of PLA, Dalian 116021, China; 2.Shanghai Dirandancheng Pharmaceutical Co., Ltd, Shanghai 200000, China; 3.Shenyang E-living Medical Technology Co., Ltd, Shenyang 110179, China) ABSTRACT: OBJECTIVE To study the pharmacokinetics and bioequivalence of two tiopromin preparations in healthy volunteers. METHODS Tiopromin concentrations of the test and the reference tablets in plasma were determined by LC-MS/MS, the pharmacokinetic parameters were calculated by DAS software, and then their bioequivalene in healthy volunteers was studied. RESULTS The main pharmacokinetic parameters of the test and reference tablets were as follows: t1/2 were (12.8±5.3) and (10.8±4.6) min; Cmax were (7.02±1.35) and (7.16±0.81) g·mL1; AUC0-t were (44.0±8.3) and (45.5±6.5) g·h·mL1, AUC0-∞ were (50.1±10.7) and (50.7±9.5) g·h·mL1, respectively. The relative