UPLC-MS法测定大鼠血浆中荭草花的3个指标成分及其药动学研究

Pharmacokinetics of three index components in flower of Polygonumorientale L. in rat plasma by UPLC-MS

目的建立UPLC-MS法测定大鼠口服荭草花提取物后血浆中原儿茶酸、山柰素-葡萄糖、槲皮苷的分析方法,并用该方法研究原儿茶酸等3个指标成分的药物代谢动力学。方法血浆样品选择酸化后甲醇沉淀蛋白,Waters BEH C18（2.1 mm×100 mm,1.7μm）柱,流速：0.30 m L·min-1,流动相：0.1%甲酸乙腈-0.1%甲酸水梯度洗脱,采用电喷雾电离源（ESI）,扫描方式为多反应离子监测（SIR）。结果 3种成分分别在2.74-677、0.69-186、0.82-200μg·L-1呈良好线性关系。提取回收率、精密度、准确度和稳定性均良好达到测定要求。原儿茶酸、山柰素-葡萄糖和槲皮苷3个指标成分的Tmax（h）分别为0.46±0.1、0.79±0.33和2.63±4.6,Cmax（μg·L-1）分别为463.8±207.81、18.53±7.82和137.38±71.09。结论建立的UPLC-MS检测方法具有特异、快速、准确和灵敏的特点,能够同时测定生物样品中原儿茶酸等3种成分的血药浓度,并成功应用于荭草花在正常大鼠体内这3个指标成分的药动学研究。

Aims To establish a UPLC-MS method for quantifying protocatechuie acid,kaempferol-3-O-β-Dglucoside and quercitrin and to investigate the pharmacokinetics of three indix components in flower of Polygonumorientale L. in rat plasma. Methods The analysis was achieved by BEH C18column（ 2. 1 mm × 100 mm,1. 7 μm） with a mobile phase composed of 0. 1%formic acid using step gradient elution. A TQD tandem mass spectrometry equipped with electrospray ionization source was used as detector and operated by selected ion recording（ SIR） mode. Results In the selected linear range,calibration curves of the three markers components showed good linearity. Extraction recovery rate,precision,accuracy and stability reached the determination request. The parameters of Tmax（ h） in three index components were 0. 46 ± 0. 1,0. 79 ± 0. 33 and 2. 63 ± 4. 6,respectively; Cmax（ μg·L- 1） in three index components were 463. 8 ± 207. 81,18. 53 ± 7. 82 and 137. 38 ± 71. 09,respectively. Conclusion The fully validated UPLC-MS method has been successfully applied to the pharmacokinetic study of the three index components in flower of Polygonumorientale L. in rat plasma.