Li Cuiyun, Ding Yanhua, Yang Deming, Wang Meng, Hu Yue, Zhang Hong, Zhu Xiaoxue, Chen Guiling, Li Xiaojiiao, Wu Min, Liu Jingrui, Chen Hong, Liu Chengjiao, Shen Zhenwei, Liu Bin
Int J Clin Pharmacol Ther. 2018 Nov;56(11):562-570. doi: 10.5414/CP203295.
This study was designed to evaluate the pharmacokinetic (PK) properties and bioequivalence (BE) of two 250-mg tablet formulations of abiraterone acetate: a newly developed generic formulation (test) and a branded formulation (reference) in healthy adult Chinese subjects under fasted (n = 40) and fed (n = 40) conditions.
The comparison was performed using a single-dose, open, randomized, and four-way replicate study. The concentration of abiraterone in blood samples taken over 48 hours was determined by liquid chromatography tandem mass spectrometry (LC-MS/MS). To assess the BE of the test and reference formulations, confidence intervals (CI, 90%) for the peak plasma concentration (C) and area under the concentration-time curves (AUC and AUC) were calculated using the reference-scaled average bioequivalence (RSABE) method.
The results showed that the 90% CIs for the ratios of C, AUC, and AUC in the fasted study were 90.14 - 114.11, 93.96 - 115.07, and 93.72 - 113.331, respectively. For the fed study, the 90% CIs were 81.83 - 102.51, 91.51 - 104.89, and 91.46 - 104.58, respectively.
CONCLUSION: In conclusion, the tested 250-mg abiraterone tablets were bioequivalent to 250-mg Zytiga tablets (reference) under both fasted and fed conditions. In addition, food intake increased the systemic exposure and C of abiraterone by 3-fold and 7-fold, respectively. .
本研究旨在评估两种250毫克醋酸阿比特龙片剂制剂的药代动力学（PK）特性和生物等效性（BE）：一种新开发的仿制药制剂（试验品）和一种品牌制剂（参比品），在健康成年中国受试者的空腹（n = 40）和进食（n = 40）条件下进行研究。
采用单剂量、开放、随机和四交叉重复研究进行比较。通过液相色谱串联质谱法（LC-MS/MS）测定48小时内采集的血样中阿比特龙的浓度。为评估试验品和参比品制剂的生物等效性，使用参比品标化平均生物等效性（RSABE）方法计算血浆峰浓度（C）和浓度-时间曲线下面积（AUC和AUC）的置信区间（CI，90%）。
结果显示，空腹研究中C、AUC和AUC比值的90% CI分别为90.14 - 114.11、93.96 - 115.07和93.72 - 113.331。进食研究中，90% CI分别为81.83 - 102.51、91.51 - 104.89和91.46 - 104.58。
总之，受试的250毫克阿比特龙片剂在空腹和进食条件下均与250毫克泽珂片（参比品）生物等效。此外，进食使阿比特龙的全身暴露量和C分别增加了3倍和7倍。
