BIOAVAILABILITY AND PHARMACOKINETICS OF ANASTROZOLE IN HEALTHY MALE VOLUNTEERS  

作　　者：安富荣 崔岚 刘晓琰 王平全 祝德秋 曹惠明 

机构地区：[1]BaseforDrugClinicalTrial,DepartmentofClinicalPharmacologyandPharmacy,RenjiHospital,SSMU,Shanghai200001,China

出　　处：《Journal of Shanghai Second Medical University(Foreign Language Edition)》2002年第2期91-95,共5页上海第二医科大学学报（英文版）

摘　　要：Objective To evaluate bioavailability and pharmacokinetics of domestic and imported anastrozole tablets.Methods Twenty Chinese healthy male volunteers were enrolled in a randomized crossover study with a single oral dose of 2mg of the two formulations respectively. The anastrozole in plasma was measured by gas chromatography with electron-capture detection. The linear range was 1. 325-106ng /ml plasma. The extraction recovery rates for plasma concentration of 5.3, 21.2 and 53. 0ng/ml were 76.8%,87.0% and 78.7%, respectively. Inter-day and intra-day precisions of the method were < 9%. Area underconcentration-time curve ( AUC0-1), maximum plasma concentration (Cmax) and reach peak time (Tmax) were 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 main pharmacokinetic parameters of domestic and imported anastrozloe tablets such as Cmax, Tmax, AUC0 - 1 and T1/2β were (36.5± 6.9) ng /ml and (35.6±9.4)ng/ml, (1.56 ±0.41)h and(1.53 ±0.49)h, (1403.6± 321.2)ng·h/ml and (1371.6±329.4)ng.h/ml, ( 42.57 ±10.15) h and ( 43.41 ±8.59 ) h, respectively, and there were no significant differences be-tween the two formulations. Conelusion Domestic and imported anastrozole tablets were of bioequivalence.The relative bioavailability of the domestic tablet was ( 102.7± 5.6 )%.

关 键 词：阿那曲唑 抗肿瘤药物 生物利用度 药物代谢动力学 

分 类 号：R979.1[医药卫生—药品]