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Abstract：
Erigeron breviscapus, a traditional Chinese medicine, is clinically used for the treatment of occlusive cerebral vascular diseases. We developed a sensitive and reliable ultra-performance liquid chromatography-electrospray-tandem mass spectrometry (UPLC-ESI-MS/MS) method for simultaneous quantitation of chlorogenic acid, scutellarin, and scutellarein, the main active constituents in Erigeron breviscapus, and compared the pharmacokinetics of these active ingredients in sham-operated and middle cerebral artery occlusion (MCAO) rats orally administrated with Erigeron breviscapus extract. Plasma samples were collected at 15 time points after oral administration of the Erigeron breviscapus extract. The levels of chlorogenic acid, scutellarin, and scutellarein in rat plasma at various time points were determined by a UPLC-ESI-MS/MS method, and the drug concentration versus time plots were constructed to estimate pharmacokinetic parameters. The concentration of chlorogenic acid in the plasma reached the maximum plasma drug concentration in about 15 min and was below the limit of detection after 4 h. Scutellarin and scutellarein showed the phenomenon of multiple absorption peaks in sham-operated and MCAO rats, respectively. Compared with the sham-operated rats, the terminal elimination half-life of scutellarein in the MCAO rats was prolonged by more than two times and the area under the curve of each component in the MCAO rats was significantly increased. The results showed chlorogenic acid, scutellarin, and scutellarein in MCAO rats had higher drug exposure than that in sham-operated rats, which provided a reference for the development of innovative drugs, optimal dosing regimens, and clinical rational drug use.
摘要：
灯盏细辛,中药，临床上用于治疗闭塞性脑血管疾病。我们开发了一种灵敏可靠的超高效液相色谱-电喷雾-串联质谱（UPLC-ESI-MS/MS）方法，用于同时定量绿原酸，scutellarin,还有Scutellarein,灯盏花的主要活性成分，并比较了这些活性成分在口服灯盏细辛提取物的假手术和大脑中动脉闭塞（MCAO）大鼠中的药代动力学。在口服施用灯盏花提取物后的15个时间点收集血浆样品。绿原酸的含量,scutellarin,通过UPLC-ESI-MS/MS方法测定大鼠血浆中不同时间点的黄芩苷，构建药物浓度与时间的关系图来估计药代动力学参数。血浆中绿原酸的浓度在约15分钟内达到最大血浆药物浓度，4小时后低于检测限。黄芩苷和黄芩苷在假手术和MCAO大鼠中表现出多个吸收峰的现象，分别。与假手术大鼠相比，MCAO大鼠中黄芩苷的终末消除半衰期延长了两倍以上，并且MCAO大鼠中每种成分的曲线下面积显着增加。结果表明,绿原酸,scutellarin,MCAO大鼠的黄芩苷药物暴露量高于假手术大鼠，为创新药物的开发提供参考,最佳给药方案，和临床合理用药。
