目的 評價(jià)阿普斯特片受試制劑和參比制劑在健康受試者中的生物等效性。方法 采用單中心、隨機(jī)、開放、兩制劑、兩序列、兩周期交叉設(shè)計(jì)。受試者空腹或餐后口服30 mg阿普斯特片受試制劑或參比制劑,清洗期為7 d。采用HPLC-MS/MS法測定人血漿中阿普斯特,采用Phoenix WinNonlin軟件(8.2版本)進(jìn)行藥動(dòng)學(xué)參數(shù)的計(jì)算,根據(jù)每個(gè)受試者的個(gè)體血藥濃度,采用非房室模型計(jì)算阿普斯特的藥動(dòng)學(xué)參數(shù)。結(jié)果 阿普斯特片空腹和餐后試驗(yàn)受試制劑和參比制劑的主要藥動(dòng)學(xué)參數(shù)峰濃度(C_max)、藥時(shí)曲線下面積(AUC_0-t)、AUC_0-∞的幾何均值比的90%置信區(qū)間均落在80.00%~125.00%等效區(qū)間。結(jié)論 阿普斯特片受試制劑和參比制劑在健康受試者空腹和餐后狀態(tài)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