枸橼酸他莫昔芬分散片在健康人体的药动学和生物等效性研究

Pharmacokinetics and bioequivalence of citric acid tamoxifen dispersible tablet in healthy volunteers

目的:研究枸橼酸他莫昔芬分散片在健康人体内的药动学和生物等效性。方法:采用随机自身对照双周期交叉试验设计,20名男性健康志愿者口服受试制剂和参比制剂各20mg,用高效液相荧光法测定他莫昔芬的血药浓度,用非房室模型计算他莫昔芬的药动学参数。结果:枸橼酸他莫昔芬分散片和普通片的药动学参数如下:tmax分别为(6.3±2.2)、(6.7±2.4)h,Cmax分别为(72±14)、(68±16)μg/L,AUC(0-492)分别为(4.6±2.0)、(4.6±2.0)mg.L-1.h,t1/2分别为(143±24)、(153±33)h。枸橼酸他莫昔芬分散片相对于普通片的相对生物利用度为(101±13)%。结论:两制剂在人体内生物等效。

AIM： To study the pharmacokinetics and relative bioavailability of citric acid tamoxifen dispersible tablet in Chinese healthy volunteers. METHODS： In a randomized two period crossover study, 20 healthy volunteers received tested and reference tablets 20 mg. The plasma concentrations of tamoxifen were determined by HPLC. The pharmacokinetics of tamoxifen was estimated by the non-compartment model. RESULTS： The main pharmacokinetics parameters of tested and reference tablets were as the following： tmax （6.3±2.2）,（6.7±2.4） h; Cmax （72±14） , （68±16） μg/L; AUC（0-492） （4.6 ±2.0）, （4.6 ± 2.0） mg·L^-1·h; t 1/2 （ 143 ± 24）, （ 153 ± 33 ） h, respectively. The relative bioavailability was （101 ±13）%. CONCLUSION： The two formulations are bioequivalent in human.