Phase I Center of Clinical Trial, The First Affiliated Hospital of Shenzhen University, Shenzhen Second People's Hospital, Shenzhen, China.
Livzon Pharmaceutical Group Inc, Shenzhen, Guangdong Province, China.
Biomed Chromatogr. 2023 Jun;37(6):e5613. doi: 10.1002/bmc.5613. Epub 2023 Mar 27.
Fluvoxamine is a selective serotonin reuptake inhibitor commonly used for various types of depression. The purpose of this study was to evaluate the pharmacokinetics and bioequivalence of fluvoxamine maleate tablets orally on an empty stomach and after a meal in healthy adult Chinese subjects and to preliminarily evaluate their safety. A single-center, randomized, open-label, two-drug, two-period, crossover, single-dose trial protocol was designed. Sixty healthy Chinese participants were enrolled and randomly classified into fasting (n = 30) and fed groups (n = 30). Each week, subjects took fluvoxamine maleate tablets 50 mg orally once as a test preparation or as a reference preparation on an empty stomach/after meals. To evaluate the bioequivalence of test and reference tables, the concentration of fluvoxamine maleate in the plasma of the subjects at different time points after administration was detected by liquid chromatography-tandem mass spectrometry, and pharmacokinetic parameters including the maximum plasma drug concentration (C ), the time to reach maximum concentration (T ), the area under the plasma concentration-time curve from time 0 to the last measurable concentration (AUC ) and the area under the plasma concentration-time curve from time 0 to infinity (AUC ) were calculated. Our data revealed that the 90% confidence intervals of the geometric mean ratio of the test or reference drugs for the C , AUC and AUC fell within the acceptance range for bioequivalence (92.30-102.77%). The absorption, measured by AUC, did not show a significant difference between the two groups. There were no suspected serious adverse reactions or serious adverse events over the entire trial. Our results demonstrated that the test and reference tablets were bioequivalent under fasting and fed conditions.
氟伏沙明是一种选择性 5-羟色胺再摄取抑制剂，常用于治疗各种类型的抑郁症。本研究旨在评估健康成年中国受试者空腹和餐后口服马来酸氟伏沙明片的药代动力学和生物等效性，并初步评估其安全性。采用单中心、随机、开放标签、两制剂、两周期、交叉、单剂量试验方案。共纳入 60 例健康中国受试者，并随机分为空腹组（n = 30）和进食组（n = 30）。每周受试者分别空腹/餐后单次口服马来酸氟伏沙明片 50 mg 作为试验制剂或参比制剂。通过液相色谱-串联质谱法检测受试者给药后不同时间点马来酸氟伏沙明的血浆浓度，计算药代动力学参数，包括最大血浆药物浓度（C ）、达峰时间（T ）、从 0 到最后可测量浓度的血浆浓度-时间曲线下面积（AUC ）和从 0 到无穷大的血浆浓度-时间曲线下面积（AUC ），以评估试验制剂和参比制剂的生物等效性。我们的数据显示，C 、AUC 和 AUC 的试验或参比药物的几何均数比值的 90%置信区间落在生物等效性接受范围内（92.30-102.77%）。两组间 AUC 测定的吸收无显著差异。整个试验过程中均未发生可疑严重不良反应或严重不良事件。我们的结果表明，在空腹和进食条件下，试验制剂和参比制剂具有生物等效性。
