国产盐酸托莫西汀胶囊在健康人体的生物等效性  

Bioequivalence of atomoxetine hydrochloride in Chinese health volunteers

作　　者：魏计超[1] 刘西哲[1] 于洋[2] 侯艳宁[2] 

机构地区：[1]河北医科大学第三医院药剂科,石家庄市050051 [2]白求恩国际和平医院国家药品临床研究机构,石家庄市050082

出　　处：《临床合理用药杂志》2015年第14期3-5,共3页Chinese Journal of Clinical Rational Drug Use

摘　　要：目的建立人血浆中托莫西汀浓度的HPLC-MS/MS测定方法,研究国产盐酸托莫西汀胶囊在中国健康男性志愿者的主要药动学参数及与参比制剂的生物等效性。方法采用两试剂双周期交叉试验设计,24名健康受试者分别单剂量口服受试制剂和参比制剂20mg,采用LC-MS/MS法测定血浆中托莫西汀的浓度,DAS 2.1.1软件计算药动学参数并考察生物等效性。结果受试制剂和参比制剂在受试者体内的药动学参数如下:Cmax分别为(232.5±86.9)和(222.8±101.1)ng/ml;tmax分别为(1.17±1.14)和(1.27±1.09)h;t1/2分别为(3.55±1.33)和(3.38±1.2)h;AUC0-t分别为(1 610±1 329)和(1 575±1 301)ng·ml-1·h-1;AUC0-∞分别为(1 683±1 466)和(1 634±1 392)ng·ml-1·h-1;受试制剂对参比制剂的相对生物利用度为(104.9±14.3)%。结论两制剂具有生物等效性。Objective To establish a method for determination of atomoxetine plasma concentration by HPLC-MS/MS and study the bioavailability and bioequivalence of atomoxetine capsule in Chinese health male volunteers. Methods A randomized,two periods,crossover bioequivalence trial was designed. 24 healthy volunteers were randomly divided into two groups,and they were given a single oral dose of the tested atomoxetine capsule and reference atomoxetine capsule 20 mg respectively. The concentrations of atomoxetine in plasma were determined by a valid LC-MS / MS method. The pharmacokinetic parameters and relative bioavailability were processed by DAS 2. 1. 1 program to evaluate the bioequivalence of test and reference capsule. Results The pharmacokinetic parameters of the test and reference capsules were as follows： Cmaxwere（ 232. 5 ±86. 9） and（ 222. 8 ± 101. 1） ng / ml; tmaxwere（ 1. 17 ± 1. 14） and（ 1. 27 ± 1. 09） h; t1 /2were（ 3. 55 ± 1. 33） and（ 3. 38 ±1. 20） h; AUC0- twere（ 1610 ± 1329） and（ 1575 ± 1301） ng · ml^- 1·h^- 1; AUC0- ∞were（ 1683 ± 1466） and（ 1634 ±1392） ng·ml^- 1·h^- 1,respectively. The relative bioavailability of the test capsules was（ 104. 9 ± 14. 3） %. Conclusion The two preparations were bioequivalence.

关 键 词：托莫西汀 高效液相色谱—串联质谱 生物等效性 

分 类 号：R969.1[医药卫生—药理学]