目的 评价阿普斯特片受试制剂和参比制剂在健康受试者中的生物等效性。方法 采用单中心、随机、开放、两制剂、两序列、两周期交叉设计。受试者空腹或餐后口服30 mg阿普斯特片受试制剂或参比制剂,清洗期为7 d。采用HPLC-MS/MS法测定人血浆中阿普斯特,采用Phoenix WinNonlin软件(8.2版本)进行药动学参数的计算,根据每个受试者的个体血药浓度,采用非房室模型计算阿普斯特的药动学参数。结果 阿普斯特片空腹和餐后试验受试制剂和参比制剂的主要药动学参数峰浓度(C_max)、药时曲线下面积(AUC_0-t)、AUC_0-∞的几何均值比的90%置信区间均落在80.00%~125.00%等效区间。结论 阿普斯特片受试制剂和参比制剂在健康受试者空腹和餐后状态下具有生物等效性。

Objective To evaluate the bioequivalence of test preparation and reference preparation of Apremilast Tablets in healthy subjects. Methods A single-center, randomized, open-label, two-treatment, two-sequence, two-period crossover design was used. Subjects were po administered with 30 mg Apremilast Tablets test or reference preparation on fasting or fed condition, and the washout period was 7 d. HPLC-MS/MS method was used to determine concentration of apremilast in human plasma. Phoenix WinNonlin software (version 8.2) was used to calculate the pharmacokinetic parameters. According to the individual plasma concentration of each subject, the pharmacokinetic parameters of apremilast were calculated by non-atrioventricular model (NCA). Results Under fasting and fed conditions, the 90% confidence intervals of the geometric mean ratios of the main pharmacokinetic parameters, such as C_max, AUC_0-t, and AUC_0-∞of test preparation and reference preparation were within the range of 80.00% to 125.00%. Conclusion The test and reference preparation of Apremilast Tablets are bioequivalent in healthy subjects on fasting or fed condition.

R927.1