国产盐酸特拉唑嗪胶囊剂的人体相对生物利用度和生物等效性评价  

The relative bioavailability and bioequivalence assessment of domestic terazosin in healthy volunteers

作　　者：吕芳玲[1] 许风云 黄跃华[1] 张远[1] 

机构地区：[1]北京医科大学药理学系,北京100083

出　　处：《北京医科大学学报》1999年第6期558-561,共4页Journal of Peking University(Health Sciences)

摘　　要：目的：研究国产特拉唑嗪胶囊剂的人体相对生物利用度和生物等效性。方法：９ 名男性健康志愿者口服国产盐酸特拉唑嗪胶囊剂和进口片剂，用高效液相色谱法测定血浆中特拉唑嗪（质量） 浓度，按照随机、交叉试验设计给药。在取血同时测量血压和心率。结果：口服国产胶囊剂和进口片剂的药时曲线均符合二室模型，ρｍａｘ 分别为（４１±１１）、（４４ ±１０） μｇ·Ｌ－ １ ，ｔｍａｘ（０ ．８±０．４）和（０ ．７±０．５） ｈ；ｔ１／２（１２±４） 和（９．０ ±１．６） ｈ；ＡＵＣо∝（４０５±１０６） 和（３９８ ±９０） μｇ·ｈ·Ｌ－ １ ， 经统计学处理两种制剂的药代动力学参数差异无显著性（ Ｐ＞ ０．０５） 。国产特拉唑嗪胶囊剂的相对生物利用度为１０４ ．４３ ％ 。双单侧检验表明：两种制剂生物等效。药效学提示血药（ 质量） 浓度达高峰时，血压稍降但不明显，心率无明显变化，两制剂间差异无显著性。结论：（１） 两制剂的药代动力学参数差异无显著性（Ｐ＞ ０ ．０５） ，国产胶囊剂生物利用度１０４．４３％ ；（２） 特拉唑嗪国产胶囊剂和进口片剂生物等效；（３）正常人单次口服２ｍｇ 特拉唑嗪胶囊剂或片剂对血压、心率无明显影响。Objective:The pharmacokinetics and pharmacodynamics of terazosin domestic capsules and imported tablets in 9 normal male healthy volunteers were studied. Method: Drug concentration in plasma was determined by HPLC. Results: The plasma concentration time curve of the domestic capsules and imported tablets were all fitted to two compartment model. ρ max were (41±11) and (44±10) μg·L -1 ; t max (0.8±0.4) and (0.7±0.5) h; t 1/2 (12±4) and (9.0±1.6) h; AUC 0 ∝ (405±106) and (398±90) μg·h·L -1 , respectively. The relative bioavailability of domestic capsules was 104.43%. The study of pharmacodynamics revealed blood pressure reduced lightly, and there was no significant changes in the heart rate of two preparations .The statistical analysis showed that there was no significant difference between the two preparations ( P >0.05). Conclusion: (1) F of terazosin capsules was 104.43%. (2) Domestic capsules and imported tablets were bioequivalent. (3) There were no significant changes in the blood pressure and heard rate in normal male volunteers after a single oral dose (2 mg) of two terazosin preparations.

关 键 词：特拉唑嗪 生物利用率 胶囊剂 降压药 

分 类 号：R972.4[医药卫生—药品] R969.1[医药卫生—药学]