枸橼酸他莫昔芬胶囊的人体生物等效性  

Bioequivalence of tamoxifen citrate capsules in healthy volunteers

作　　者：师少军[1] 李忠芳[1] 徐顺清[2] 陈笑艳[3] 钟大放[3] 陈华庭[1] 曾繁典[2] 

机构地区：[1]华中科技大学同济医学院附属协和医院,湖北武汉430022 [2]华中科技大学同济医学院临床药理研究所,湖北武汉430030 [3]中国科学院上海药物研究所药物代谢研究中心,上海201203

出　　处：《中国医院药学杂志》2008年第19期1668-1672,共5页Chinese Journal of Hospital Pharmacy

摘　　要：目的:研究枸橼酸他莫昔芬胶囊在人体的相对生物利用度和生物等效性。方法:20名健康男性受试者,采用双周期交叉、自身对照试验设计,分别单剂量口服枸橼酸他莫昔芬受试和参比制剂各40mg,采用液相色谱-串联质谱法测定其血药浓度,应用DAS软件计算药动学参数和相对生物利用度,评价2种制剂的生物等效性。结果:枸橼酸他莫昔芬受试和参比制剂的主要药动学参数:t1/2分别为(53.5±14.4)h和(51.7±8.9)h;tmax分别为(3.9±0.9)h和(4.0±1.1)h;Cmax分别为(108.1±19.8)μg.L-1和(101.3±16.5)μg.L-1;AUC0-72分别为(3 073.7±439.1)μg.h.L-1和(3148.8±373.7)μg.h.L-1;AUC0-∞分别为(5 074.8±1 082.2)μg.h.L-1和(5 121.2±902.0)μg.h.L-1。方差分析结果表明,2种制剂的主要药动学参数之间差异无显著性。枸橼酸他莫昔芬受试制剂的相对生物利用度为(97.9±10.8)%。结论:经统计学分析,两种制剂具有生物等效性。OBJECTIVE To evaluate the relative bioavailability and bioequivalence of tamoxifen citrate capsules in healthy volunteers. METHODS A single oral close of 40 mg tamoxifen citrate test and reference preparations were given to 20 male healthy volunteers in a randomized crossover design. Tamoxifen concentrations in plasma were determined by LC/MS/MS. The pharmacokinetic parameters and relative bioavailability were calculated with DAS program to evaluate the bioequivalence of the two preparations. RESULTS The main pharmacokinetic parameters of tamoxifen citrate test and reference preparations were as follow, t1/2were （53. 5 ± 14. 4） h and （51.7 ± 8. 9） h; tmax were （3. 9 ± 0. 9） h and （4. 0 ± 1.1） h; Cmax were （108. 1 ± 19. 8）μg·L^-1 and （101.3 ± 16. 5） μg·L^-1 ; AUC0-72 were （3 073. 7 ± 439. 1 ） μg·h·L^-1 and （3 148. 8 ± 373. 7）μg·h·L^-1 AUG0-∞ were （5 074. 8 ± 1 082.2） μg·h·L^-1 and （5 121.2 ± 902. 0）μg·h·L^-1, respectively. The differences of the major pharmacokinetic parameters between test and reference preparations were not significant. The relative bioavailability of test preparation was （97.9 ± 10. 8） %. CONCLUSION The statistical analysis of the results shows that the two preparations are bioequivalent.

关 键 词：枸橼酸他莫昔芬 液相色谱-串联质谱法 生物利用度 生物等效性 

分 类 号：R969.1[医药卫生—药理学]