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目的：应用液相色谱-串联质谱法（LC-MS/MS）建立大鼠血浆中阿姆西汀（S-071031B）浓度测定方法，并考察大鼠灌胃给予阿姆西汀后的药代动力学。方法采用LC-MS/MS方法，以盐酸苯环壬酯左旋体（ L-8021）为内标，C18柱为分析柱，流动相为含0．1％甲酸的水-乙腈体系，流速为0．3 ml/min，采用电喷雾正离子（ESI ＋）、选择反应监测（SRM）模式进行检测。绘制血药浓度-时间曲线并利用DAS 2．0计算药代动力学参数。结果大鼠血浆中内源性杂质不干扰阿姆西汀和内标的测定，阿姆西汀的线性范围为2～1000 ng/ml （r2＝0．9965），定量限为2 ng/ml，日内、日间精密度和准确度，绝对回收率和基质效应均符合生物样品测定需要。大鼠口服灌胃后在（0．8±0．3）h达到（287．2±50．8）μg/L的峰值浓度，t1/2为（2．9±0．6）h，AUC（0-∞）为（1372．6±255．3）μg/L· h。结论本方法灵敏度高、特异性好，可用于血浆中阿姆西汀的浓度测定及其药代动力学研究。“,”Objective To establish an LC-MS/MS method for determination of S-071031 B, a novel antidepressant , in rat plasma and to study its pharmacokinetic profiles .Methods An LC-MS/MS method was established to determine S-071031B in rat plasma, and L-8021 was employed as the internal standard .The analytes were separated on a C18 column with a mobile phase consisting of water-acetonitrile containing 0.1%(v/v) formic acid at a flow rate of 0.3 ml/min.The mass spectrometer was operated in a selected reaction monitoring ( SRM ) mode with a positive electrospray ionization (ESI) interface.The plasma concentration-time curve was drawn and pharmacokinetic parameters were calculated by DAS 2.0.Results The linear range was from 2 to 1000 ng/ml with a sensitivity of 2 ng/ml as the lower limit of quantification . The intra-day and inter-day precisions , recoveries and matrix effects at three spiked levels were all suited to the determina-tion of biological samples.After oral administration of S-071031B, the Cmax of S-071031B was (287.2 ±50.8) μg/L and the Tmax was (0.8 ±0.3) h, with a t1/2of (2.9 ±0.6) h and an AUC(0-∞)of (1372.6 ±255.3) μg/L· h.Conclusion This method is sensitive and specific enough for determination of S-071031 B in rat plasma to facilitate the study of its phar-macokinetics .