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目的:建立木犀草素血药浓度的高效液相色谱测定方法,并探讨其在大鼠体内的药动学行为。方法:采用Agilent TC-C18(4.6mm×150mm,5μm)色谱柱,以乙腈-0.5mol·L-1磷酸二氢钾溶液(40∶60)为流动相,流速1.0mL.min-1,检测波长280nm。大鼠灌胃木犀草素30mg·kg-1后,于不同时间点断尾采血,用HPLC法测定其血药浓度,经3P97药动学计算程序处理,得到药动学参数。结果:大鼠血浆中,木犀草素的线性范围为20～1200ng·mL-1(r=0.9967),方法回收率大于96%,最低检测限为15ng·mL-1。大鼠灌胃木犀草素后,木犀草素的血药浓度-时间变化曲线符合二室模型,Tmax为(0.732±0.13)h,Cmax为(0.691±0.14)mg·mL-1,AUC为(0.435±0.12)mg·h·mL-1。结论:本试验建立的大鼠血浆中木犀草素含量的HPLC测定方法,专属性强,灵敏度高,可用于该药在大鼠体内的药代动力学研究。
OBJECTIVE: To establish a HPLC method for determination of luteolin in plasma and investigate its pharmacokinetics in rats. Methods: The mobile phase was acetonitrile-0.5mol·L-1 potassium dihydrogen phosphate solution (40:60) with a flow rate of 1.0mL · min-1 on an Agilent TC-C18 column (4.6mm × 150mm, 5μm) Wavelength 280nm. Rats were administered with luteolin (30 mg · kg-1), and the blood samples were collected from the tail at different time points. The plasma concentration of the drug was determined by HPLC. Pharmacokinetic parameters were obtained by 3P97 pharmacokinetic calculation. Results: The linear range of luteolin in rat plasma was 20 ~ 1200 ng · mL-1 (r = 0.9967). The recovery of the method was more than 96%. The lowest detection limit was 15 ng · mL-1. After administration of luteolin in rats, the concentration-time curve of luteolin conformed to the two-compartment model with a Tmax of (0.732 ± 0.13) h and a Cmax of (0.691 ± 0.14) mg · mL- 0.435 ± 0.12) mg · h · mL-1. Conclusion: The method for the determination of luteolin in plasma of rats established by this method has high specificity and high sensitivity and can be used for the pharmacokinetic study of this drug in rats.