Lei Yuyan, Yan Yu, Lu Junli, Li Chao, Wang Jie, Li Canxia, Huang Lifeng, Wang Caihong, Liu Wanying, Li Xiaohui, Chen Weiming, Xia Man, Chen Lulu
Phase I, Clinical Trial Laboratory, The Second Nanning People's Hospital, Nanning, China.
Department of Pharmacology, School of Pharmaceutical Science, Central South University, Changsha, China.
Clin Pharmacol Drug Dev. 2024 Jan;13(1):103-110. doi: 10.1002/cpdd.1331. Epub 2023 Sep 23.
Blonanserin is a novel oral antischizophrenic drug. Under fasting (n = 50) and fed (n = 60) conditions, this study compared the bioequivalence of the generic blonanserin tablet with the reference blonanserin tablet. In this single-center, randomized, open-label, 2-period, 2-sequence, crossover study, 110 patients were randomly given a 4-mg dose of either the test or reference blonanserin tablet with a 14-day washout period. Blood samples were taken before performing and up to 72 hours following. A validated high-performance liquid chromatography-tandem mass spectrometry technique was used to measure the levels of blonanserin in plasma. Safety was evaluated throughout the study. The study found no significant differences in the maximum observed drug concentration in the plasma (C ), the area under the plasma concentration-time curve from time 0 to the last sampling time (AUC ), and the area under the plasma concentration-time curve from time 0 to infinity (AUC ) between the 2 blonanserin formulations. The 90% confidence intervals of the geometric mean ratio of the test/reference formulations for C , AUC , and AUC were within the 80%-125% limit. Food dramatically raised blonanserin exposure, and also significantly prolonged the lag time of absorption. No serious adverse events occurred. These results indicate that the 2 blonanserin formulations were bioequivalent and well tolerated in healthy Chinese subjects. In clinical treatment, it is necessary to consider the food effect of blonanserin.
布南色林是一种新型口服抗精神分裂症药物。在空腹（n = 50）和进食（n = 60）条件下，本研究比较了布南色林仿制药片与参比布南色林片的生物等效性。在这项单中心、随机、开放标签、两期、两序列、交叉研究中，110名患者被随机给予4毫克剂量的试验用或参比布南色林片，洗脱期为14天。在给药前及给药后长达72小时采集血样。采用经过验证的高效液相色谱 - 串联质谱技术测量血浆中布南色林的水平。在整个研究过程中评估安全性。研究发现，两种布南色林制剂在血浆中观察到的最大药物浓度（Cmax）、从时间0至最后采样时间的血浆浓度 - 时间曲线下面积（AUC0 - t）以及从时间0至无穷大的血浆浓度 - 时间曲线下面积（AUC0 - ∞）方面无显著差异。试验/参比制剂的Cmax、AUC0 - t和AUC0 - ∞几何平均比值的90%置信区间在80% - 125%范围内。食物显著提高了布南色林的暴露量，并且还显著延长了吸收的滞后时间。未发生严重不良事件。这些结果表明，两种布南色林制剂在健康中国受试者中具有生物等效性且耐受性良好。在临床治疗中，有必要考虑布南色林的食物效应。
