目的 建立超高效液相色谱-质谱（UPLC-MS/MS）同时测定大鼠血浆中苦参酮（Kur）、槐属二氢黄酮G（SFG）和异黄腐醇（Iso）3个成分的分析方法，研究苦参总黄酮（TF）及苦参总黄酮自微乳（TF-SMEDDS）在大鼠体内的药动学过程和药动学参数。方法 色谱柱采用ACQUITY UPLC^® HSS T3 C₁₈，流动相为乙腈-0.1%甲酸水梯度洗脱，体积流量0.2 mL/min，待测血浆样品采用醋酸乙酯液-液萃取法制备。电喷雾离子化电离源（ESI）以多反应离子监测（MRM）模式进行负离子方式检测，芦丁为内标（IS），DAS 2.0软件处理数据。结果 TF提取物中Kur、SFG、Iso分别在（0.02~1 600.00）、（0.015~1 200.000）、（0.01~800.00）ng/mL有良好的线性关系（r²均大于0.995 9）；精密度、准确度、平均提取回收率以及基质效应等均符合生物样品分析要求。TF给药后，Kur、SFG和Iso的半衰期（t_1/2z）分别为（7.04±2.46）、（4.54±2.13）、（4.73±1.67）h，药时曲线下面积（AUC_0~∞）分别为（3 469.57±555.37）、（2 524.48±425.83）、（1 006.47±85.46）ng·h/mL；TF-SMEDDS给药后，Kur、SFG和Iso的t_1/2z分别为（13.10±2.67）、（11.47±4.17）、（12.67±4.97）h，AUC_0~∞分别为（13 002.49±2 498.09）、（8 070.80±2 264.62）、（3 918.85±429.76）ng·h/mL。TF-SMEDDS中Kur、SFG和Iso的相对生物利用度分别为374.76%、319.70%、389.37%。结论 所建立的UPLC-MS/MS分析方法可用于苦参中3个成分在大鼠体内药动学研究，制成自微乳后能够显著提高TF在大鼠体内的生物利用度。

Objective To establish a UPLC-MS/MS method for simultaneous determination of sophoraflavanone G (SFG), kurarinone (Kur), and isoxanthohumol (Iso) in rat plasma using rutin as the internal standard (IS), and to study the pharmacokinetic parameters of total flavonoids (TF) from Sophora flavescens and TF self-microemulsion drug delivery system (TF-SMEDDS) in rats. Methods Analysis was carried out on an ACQUITY UPLC^® HSS T3 C₁₈ column using acetonitrile-0.1% formic acid in water as the mobile phase at a flow rate of 0.2 mL/min. The plasma samples were prepared by liquid-liquid extraction with ethyl acetate. The detection was performed on a triple quadrupole tandem mass spectrometer by multiple reaction monitoring with an electro-spray ionization source in negative ionization mode. All statistical analysis was performed using DAS 2.0 software package. Results The calibration curves of Kur, SFG, and Iso exhibited good linearity (r² > 0.995 9) over the range of (0.02-1 600.00), (0.015-1 200.000), and (0.01-800.00) ng/mL, respectively. Precision, accuracy, average extraction recovery, and matrix effects were all in line with biological sample analysis requirements. The pharmacokinetic parameters of Kur, SFG, and Iso from TF were as follows:t_1/2z (7.04 ±2.46), (4.54 ±2.13), (4.73 ±1.67) h, and AUC_0-∞ (3 469.57 ±555.37), (2 524.48 ±425.83), (1 006.47 ±85.46) ng·h/mL. The pharmacokinetic parameters of Kur, SFG, and Iso from TF-SMEDDS were as follows:t_1/2z (13.10 ±2.67), (11.47 ±4.17), and (12.67 ±4.97) h, and AUC_0-∞ (13 002.49 ±2 498.09), (8 070.80 ±2 264.62), (3 918.85 ±429.76) ng·h/mL. The relative bioavailabilities of Kur, SFG, and Iso in TF-SMEDDS were approximately 374.76%, 319.70%, and 389.37%, respectively. Conclusion The UPLC-MS/MS method can be used to study the pharmacokinetics of three components in S. flavescens in rats. The bioavailability of TF-SMEDDS in rats was significantly increased.

黑龙江省自然科学基金项目（H2016057）；黑龙江省自然科学基金项目（H2017066）；黑龙江中医药大学“优秀创新人才支持计划”项目（2012，2018）；国家教育部春晖计划（Z2008-1-15016）