Wang Min, Peng Yu, Yan Hegui, Pan Zhixiang, Du Ronghui, Liu Guan
Phase I Clinical Trial Centre, Wuhan Pulmonary Hospital, Wuhan Institute of Tuberculosis Prevention and Control, Wuhan, 430030, Hubei Province, China.
Drugs R D. 2025 Apr 26. doi: 10.1007/s40268-025-00508-7.
Amisulpride is a second-generation antipsychotic drug that selectively binds to D2 and D3 dopaminergic receptors in the limbic system. In this study, the bioequivalence of an amisulpride formulation manufactured in China with the original formulation Solian® was evaluated under fasting and fed conditions in healthy Chinese subjects.
A single-centre, randomized, open, two-preparation, single-dose, two-period crossover trial in healthy adult subjects was conducted under fasting and fed conditions. A total of 42 and 36 eligible healthy subjects were enrolled in the fasting and fed studies, respectively. The subjects were randomly assigned to receive either the test or the reference formulation with a washout period of 7 days. The concentration of amisulpride in plasma was determined by liquid chromatography‒tandem mass spectrometry (LC‒MS/MS), and the pharmacokinetic (PK) parameters of amisulpride were calculated via the noncompartmental method.
The geometric mean ratios (GMR) of the maximum observed concentration (C), the area under the plasma concentration‒time curve (AUC) from time zero to the last sampling time (AUC), and the AUC from time zero to infinity (AUC) from the test/reference formulation under fasting conditions were 93.83, 101.90, and 102.35, respectively, with corresponding 90% confidence intervals (CIs) of 83.93-104.89, 97.58-106.42, and 98.24-106.63. The GMRs of C, AUC, and AUC under fed conditions were 102.23, 106.09, and 101.87, respectively, with corresponding 90% CIs of 92.49-112.99, 102.44-109.87, and 97.49-106.44. These data all satisfied the bioequivalence criteria (90% CIs in the range of 80-125%). In terms of safety, no serious adverse events were observed.
The test and reference amisulpride formulations were bioequivalent under fasting and fed conditions. Both formulations showed similar safety and tolerability in the population studied.
氨磺必利是一种第二代抗精神病药物，可选择性地与边缘系统中的D2和D3多巴胺能受体结合。在本研究中，对中国生产的氨磺必利制剂与原研制剂索里昂®在健康中国受试者的空腹和进食条件下进行了生物等效性评估。
在健康成年受试者中进行了一项单中心、随机、开放、双制剂、单剂量、两周期交叉试验，试验在空腹和进食条件下进行。分别有42名和36名符合条件的健康受试者纳入空腹和进食研究。受试者被随机分配接受试验制剂或参比制剂，洗脱期为7天。采用液相色谱 - 串联质谱法（LC - MS/MS）测定血浆中氨磺必利的浓度，并通过非房室方法计算氨磺必利的药代动力学（PK）参数。
空腹条件下试验/参比制剂的最大观测浓度（C）、血浆浓度 - 时间曲线下从零至最后采样时间的面积（AUC）以及从零至无穷大的AUC的几何平均比值（GMR）分别为93.83、101.90和102.35，相应的90%置信区间（CI）分别为83.93 - 104.89、97.58 - 106.42和98.24 - 106.63。进食条件下C、AUC和AUC的GMR分别为102.23、106.09和101.87，相应的90%CI分别为92.49 - 112.99、102.44 - 109.87和97.49 - 106.44。这些数据均符合生物等效性标准（90%CI在80% - 125%范围内）。在安全性方面，未观察到严重不良事件。
试验和参比氨磺必利制剂在空腹和进食条件下具有生物等效性。两种制剂在所研究人群中显示出相似的安全性和耐受性。
