Pharmacokinetics of anastrozole in Chinese male volunteers  

阿那曲唑在中国男性志愿者体内的药代动力学

作　　者：袁静[1] 王平全[1] 戈升荣[1] 安富荣[1] 施安国[1] 陈钧[2] 梁建英[2] 

机构地区：[1]上海第二医科大学附属仁济医院临床药学药理研究室,国家药品临床研究基地,上海中国200001 [2]上海医科大学药物分析教研室,上海中国200032

出　　处：《Acta Pharmacologica Sinica》2001年第6期97-100,共4页中国药理学报（英文版）

摘　　要：AIM: To compare pharmacokinetics of domestic and imported tablets of anastrozole. METHODS: Twenty male Chinese volunteers were enrolled in a randomized crossover study with a single oral dose of 1 mg of the two formulations respectively. The anastrozole in plasma was measured by gas chromatography with electron-captured detector. Area under the drug concentration-time curve was evaluated by variance analysis and two one-side t-test. RESULTS: A two-compartment model was adopted in anastrozole plasma concentration-time data analysis. The paramaters such as Cmax, Tmax, T1/2β, and AUC0-∞ were (10±3) and (10.2±2.5) μg·L-1, (1.2 ±0.5) and (1.3 ±0.4) h, (42 ±14) and (41 ± 26) h, (443±141) and (429±121) μg·h·L-1, respectively, and there were no significant differences between the two formulations. CONCLUSION: Domestic and imported anastrozole were of bioequivalence. The relative bioavailability of the domestic tablet was 100 % ± 9 %.目的:比较国产和进口阿那曲唑片在健康人体内的药代动力学。方法:二十名志愿者交叉随机分成两组,单剂量口服1mg,用GC-ECD测定血药浓度,通过方差分析和双单侧t检验比较两种制剂的药-时曲线下面积。结果:阿那曲唑的体内分布符合二室模型。国产和进口阿那曲唑的药动学参数C_(max)分别为(10±3)和(10.2±2.5)μg·L^(-1);T_(max)分别为(1.2±0.5)和(1.3±0.4)h;T_(1/2β)分别为(42±14)和(41±26)h;AUC_(0-∞)分别为(443±141)和(429±121)μg·h·L^(-1),两者无显著性差别(P>0.05)。结论:两种制剂为生物等效,国产阿那曲唑片的相对生物利用度为100％±9％。

关 键 词：ANASTROZOLE PHARMACOKINETICS gas chromatography biological availability 

分 类 号：R96[医药卫生—药理学]