健康受试者醋酸环丙孕酮片的生物等效性测定

Bioequivalent study of cyproterone acetate tablet in healthy human

目的:研究检测比较人体单次口服受试制剂醋酸环丙孕酮片和参比制剂醋酸环丙孕酮片的生物利用度。方法:18名男性健康志愿者采用两制剂双周期交叉试验设计,口服醋酸环丙孕酮片受试制剂和参比制剂各100mg,于不同时间采集血样,并采用高液相色谱法测定血药浓度。结果:受试者口服两种醋酸环丙孕酮片受试制剂和参比制剂后,T_(max)分别为(3.7±0.8)h和(3.9±0.5)h,C_(max)分别为(145.0±46.8)和(151.1±47.9)ng/ml,AUC0￣96分别为(2303.6±446.2)和(2182.2±426.5)ng/(h·ml)。醋酸环丙孕酮片受试制剂和参比制剂消除均较缓慢,消除半衰期分别为(29.4±10.3)和(26.4±7.4)h。AUC0￣96和C_(max)经对数转化后进行方差分析和双单侧t检验,T_(max)进行秩和检验,结果表明受试制剂的AUC0￣96、C_(max)和T_(max)与参比制剂比较差异无统计学意义。结论:醋酸环丙孕酮片受试制剂的人体相对生物利用度为(107.4±19.2)%,与参比制剂具有生物学等效性。

Objective：To make a comparison study of the bioavailability of test cyproterone acetate and reference cyproterone acetate by using HPLG method. Methods：In a randomized cross over study,two types of cyproterone acetate in single oral dose 100 mg each were given to 18 healthy volunteers every two weeks,and the blood tests were taken in different time.Results：The main pharmacokinetie parameters of these two types of eyproterone acetate were as follows ： Tmax was （0.6±0.12） and （0.5±0.0）h respectively;Cmax was （25.1±2.2） and （26.6±2.4）ng/ml respectively;AUC0-96 was （163.2±12.1） and （163.7±11.6）ng/h/ml respectively;The elimination half-life was （10.4±4.3） and （10.6±2.9）h respectively;Mter the logarithmic conversion of AUC0-96 and Cmax,the analysis of variance and two one sided test statistical analysis for AUC0-96 and Cmax and rank sum test for Tmax showed that two formulations had no significant difference. Conclusion：Compared with reference cyproterone acetate, the bioavailability of the test cyproterone acetate was （107.4±19.2）%. According to the statistic analysis, the two types of cyproterone acetate were bioequivalent in human.