特拉唑嗪滴丸的人体生物等效性  

Bioequivalence of terazosin pills in human

作　　者：陈钧[1] 高小玲[1] 谢月玲[1] 江文明[1] 蒋新国[1] 

机构地区：[1]复旦大学药学院药剂学教研室,上海200032

出　　处：《中国临床药学杂志》2005年第1期17-19,共3页Chinese Journal of Clinical Pharmacy

摘　　要：目的　评价单剂量口服两种特拉唑嗪制剂后的人体药动学和生物等效性。方法　采用高效液相色谱-荧光检测方法测定2 0名健康志愿者自身交叉单剂量口服特拉唑嗪滴丸和片剂2mg后的经时血药浓度。采用3P97程序计算药动学参数及相对生物利用度,评价其生物等效性。结果　2 0名受试者口服特拉唑嗪滴丸和片剂后的药动学参数分别为:tmax(0 . 93±0 . 35 )、(0 .95±0 . 39)h ;cmax(5 0 . 0±15 . 3)、(43 .2±13. 3) μg·L-1;MRT (15 . 8±2 . 0 )、(16 . 2±2 .1)h ;T1/2 (11. 3±1 .3)、(11. 4±1 .3)h ;AUC0→3 6h(433±110 )、(40 .0±10 .4 ) μg·h·L-1;AUC0→∞(479±12 .3)、(44 .3±117) μg·h·L-1。经方差分析,两种制剂的药动学参数除cmax和AUC外均无显著性差异。结论　特拉唑嗪滴丸的平均相对生物利用度为(10 9. 4 3±12 . 39) % ,特拉唑嗪滴丸和片剂生物等效。AIM To study the pharmacokinetics, relative bioavailability and bioequivalence of terazosin pills in healthy volunteers. METHODS A single oral dose of 2 mg terazosin pills and terazosin tablets was given to 20 healthy volunteers in a randomized crossover study. Terazosin concentrations in plasma were determined by HPLC with fluorescence detection. RESULTS The main pharmacokinetic parameters of the 2 formulations were as follows: t max were(0.93±0.35),(0.95±0.39) h,c max were(50.0±15.3),(43.2±13.3)μg·L -1,MRT were(15.8±2.0),(16.2±2.1 ) h,T 1/2 were(11.3±1.3 ),(11.4±1.3)h, AUC 0-36 h were(433±110),(400±104)μg·h·L -1, AUC 0-∞ were(479±123),(443±117)μg·h·L -1,respectively. There was no significant difference between the pharmacokinetic parameters except for c max and AUC according to ANOVA. CONCLUSION The relative bioavailability of terazosin pills to terazosin tablets is (109.43±12.39)%. Two-one sided t-test and the results of statistical analysis intervals test demonstrate that the 2 formulations are of bioequivalence.

关 键 词：特拉唑嗪 高效液相色谱 药动学 相对生物利用度 滴丸 

分 类 号：R96[医药卫生—药理学]