帕罗西汀片在健康人体的药动学与生物等效性

Pharmacokinetic Characteristics and Bioequivalence of Paroxetine Tablets in Healthy Chinese Volunteers

目的研究帕罗西汀片剂在健康人体的药动学过程,并比较两种帕罗西汀片剂的生物等效性。方法男性健康志愿者20例,随机交叉单剂量口服帕罗西汀片试验制剂和参比制剂40 mg后,用高效液相色谱法测定血浆帕罗西汀浓度。并用3P97药动学软件进行参数计算及评价两种制剂的生物利用度和生物等效性。结果单剂量口服试验制剂和参比制剂后血浆帕罗西汀的主要药动学参数如下:Cmax分别为(62.78±17.34)和(64.74±18.43)ng.mL-1;tmax分别为(5.13±1.37)和(5.64±1.84)h;t1/2分别为(19.85±5.72)和(20.03±5.33)h;AUC0-120分别为(1 043.21±297.33)和(1 076.47±309.49)ng.h.mL-1;AUC0-inf分别为(1 358.35±443.73)和(1 386.75±476.54)ng.h.mL-1。试验制剂与参比制剂的人体相对生物利用度为F0-120(98.9±16.3)%,F0-inf(96.3±18.2)%。结论两种帕罗西汀片剂具有生物等效性。

Objective To study the pharmacokinetic characteristics of paroxetine tablets in healthy Chinese volunteers and to compare the bioequivalence between two preparations of paroxetine tablets. Methods 20 healthy volunteers in a randomized crossover study were given each a single oral dose of 40 mg of test or reference paroxetine tablets . The plasma concentration of paroxetine was determined with HPLC. The pharmacokinetic parameters were calculated while the bioavailability and bioequivalence of the two preparations were evaluated with the 3P97 pharmacokinetic software. Results The main pharmacokinetic parameters for test and reference preparations were Cmax： （62.78±17.34） and （64.74±18.43 ） ng·mL^-1; tmax： （5.13±1.37） and （5.64±1.84） h;t1/2：（19.85±5.72） and （20.03±5.33） h;AUC0-120： （1 043.21±297.33） and （1076.47±309.49） ng·h^-1·mL^-1; AUC0-inf： （1 358.35±443.73） and （1 386.75±476.54） ng·h^-1·mL^-1, respectively. The relative bioavailability of the test and reference preparations F0-120：（98.9 ± 16.3 ）% and F0-inf： （96.3 ± 18.2） %, respectively. Conclusion The two preparations of paroxetine tablets were shown to be bioequivalent.