PDF(Pubmed)
Abstract：
UNASSIGNED: This study compared the pharmacokinetics, safety and bioequivalence (BE) of generic and original apremilast tablets in healthy Chinese subjects under fasting and postprandial conditions, providing sufficient evidence for abbreviated new drug application.
UNASSIGNED: A randomized, open-label, two-formulation, single-dose, two-period crossover pharmacokinetic study was performed. Thirty-two eligible healthy Chinese subjects were enrolled in fasting and postprandial studies, respectively. In each trial, subjects received a single 30-mg dose of the test or reference apremilast tablet, followed by a 7-day washout interval between periods. Serial blood samples were obtained for up to 48 h post-intake in each period, and the plasma concentrations of apremilast were determined by a validated method. The primary pharmacokinetic (PK) parameters, including the maximum plasma concentration (Cmax), the areas under the plasma concentration-time curve (AUC0-t, AUC0-∞), were calculated using the non-compartmental method. The geometric mean ratios of the two formulations and the corresponding 90% confidence intervals (CIs) were acquired for bioequivalence analysis. The safety of both formulations was also evaluated.
UNASSIGNED: Under fasting and postprandial states, the PK parameters of the test drug were similar to those of the reference drug. The 90% CIs of the geometric mean ratios of the test to reference formulations were 94.09-103.44% for Cmax, 94.05-103.51% for AUC0-t, and 94.56-103.86% for AUC0-∞ under fasting conditions, and 99.18-112.48% for Cmax, 98.79-106.02% for AUC0-t, and 98.95-105.89% for AUC0-∞ under postprandial conditions, all of which were within the bioequivalence range of 80.00-125.00%. Both formulations were well tolerated, and no serious adverse events occurred during the study.
UNASSIGNED: The trial confirmed that the PK parameters of the generic and original apremilast tablets were bioequivalent in healthy Chinese subjects under fasting and postprandial states, which met the predetermined regulatory standards. Both formulations were safe and well tolerated.
UNASSIGNED: chinaDrugtrials.org.cn, identifier CTR20191056 (July 30, 2019); chictr.org.cn, identifier ChiCTR2300076806 (October 19, 2023).
UNASSIGNED: A randomized, open-label, two-formulation, single-dose, two-period crossover pharmacokinetic study was performed. Thirty-two eligible healthy Chinese subjects were enrolled in fasting and postprandial studies, respectively. In each trial, subjects received a single 30-mg dose of the test or reference apremilast tablet, followed by a 7-day washout interval between periods. Serial blood samples were obtained for up to 48 h post-intake in each period, and the plasma concentrations of apremilast were determined by a validated method. The primary pharmacokinetic (PK) parameters, including the maximum plasma concentration (Cmax), the areas under the plasma concentration-time curve (AUC0-t, AUC0-∞), were calculated using the non-compartmental method. The geometric mean ratios of the two formulations and the corresponding 90% confidence intervals (CIs) were acquired for bioequivalence analysis. The safety of both formulations was also evaluated.
UNASSIGNED: Under fasting and postprandial states, the PK parameters of the test drug were similar to those of the reference drug. The 90% CIs of the geometric mean ratios of the test to reference formulations were 94.09-103.44% for Cmax, 94.05-103.51% for AUC0-t, and 94.56-103.86% for AUC0-∞ under fasting conditions, and 99.18-112.48% for Cmax, 98.79-106.02% for AUC0-t, and 98.95-105.89% for AUC0-∞ under postprandial conditions, all of which were within the bioequivalence range of 80.00-125.00%. Both formulations were well tolerated, and no serious adverse events occurred during the study.
UNASSIGNED: The trial confirmed that the PK parameters of the generic and original apremilast tablets were bioequivalent in healthy Chinese subjects under fasting and postprandial states, which met the predetermined regulatory standards. Both formulations were safe and well tolerated.
UNASSIGNED: chinaDrugtrials.org.cn, identifier CTR20191056 (July 30, 2019); chictr.org.cn, identifier ChiCTR2300076806 (October 19, 2023).
摘要：
■这项研究比较了药代动力学，在禁食和餐后条件下，在健康的中国受试者中，通用和原始的阿瑞司特片的安全性和生物等效性（BE），为简化新药应用提供充分的证据。
■随机，开放标签，两种配方，单剂量,进行了两期交叉药代动力学研究.32名符合条件的健康中国受试者参加了空腹和餐后研究，分别。在每次审判中,受试者接受单次30毫克剂量的测试或参比阿普雷斯特片剂，接下来是7天的时间间隔。在每个时期摄入后48小时内获得连续的血液样本，并通过验证的方法确定了阿普雷斯特的血浆浓度。主要药代动力学（PK）参数，包括最大血浆浓度（Cmax），血浆浓度-时间曲线下面积(AUC0-t，AUC0-∞)，使用非房室法计算。获得两种制剂的几何平均比和相应的90%置信区间(CI)用于生物等效性分析。还评估了两种制剂的安全性。
■在禁食和餐后状态下，试验药物的PK参数与参比药物相似。对于Cmax，测试配方与参考配方的几何平均比率的90％CI为94.09-103.44％，AUC0-t为94.05-103.51%，空腹条件下AUC0-∞为94.56-103.86%，Cmax为99.18-112.48%，AUC0-t为98.79-106.02%，餐后条件下AUC0-∞为98.95-105.89%，所有这些都在80.00-125.00％的生物等效性范围内。两种制剂均具有良好的耐受性，研究期间未发生严重不良事件.
■该试验证实，在空腹和餐后状态下，健康中国受试者的通用和原始阿瑞司特片的PK参数是生物等效的，符合预定的监管标准。两种制剂均安全且耐受性良好。
■chinaDrugtrials.org。cn,标识符CTR20191056（2019年7月30日）；chictr.org。cn,标识符ChiCTR2300076806（2023年10月19日）。
■随机，开放标签，两种配方，单剂量,进行了两期交叉药代动力学研究.32名符合条件的健康中国受试者参加了空腹和餐后研究，分别。在每次审判中,受试者接受单次30毫克剂量的测试或参比阿普雷斯特片剂，接下来是7天的时间间隔。在每个时期摄入后48小时内获得连续的血液样本，并通过验证的方法确定了阿普雷斯特的血浆浓度。主要药代动力学（PK）参数，包括最大血浆浓度（Cmax），血浆浓度-时间曲线下面积(AUC0-t，AUC0-∞)，使用非房室法计算。获得两种制剂的几何平均比和相应的90%置信区间(CI)用于生物等效性分析。还评估了两种制剂的安全性。
■在禁食和餐后状态下，试验药物的PK参数与参比药物相似。对于Cmax，测试配方与参考配方的几何平均比率的90％CI为94.09-103.44％，AUC0-t为94.05-103.51%，空腹条件下AUC0-∞为94.56-103.86%，Cmax为99.18-112.48%，AUC0-t为98.79-106.02%，餐后条件下AUC0-∞为98.95-105.89%，所有这些都在80.00-125.00％的生物等效性范围内。两种制剂均具有良好的耐受性，研究期间未发生严重不良事件.
■该试验证实，在空腹和餐后状态下，健康中国受试者的通用和原始阿瑞司特片的PK参数是生物等效的，符合预定的监管标准。两种制剂均安全且耐受性良好。
■chinaDrugtrials.org。cn,标识符CTR20191056（2019年7月30日）；chictr.org。cn,标识符ChiCTR2300076806（2023年10月19日）。
