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目的建立测定牛蒡苷元在大鼠血浆中药物浓度的高效液相色谱法,研究牛蒡苷元纳米乳在大鼠体内的药动学特征。方法血浆样品经乙酸乙酯萃取处理,色谱柱为Agilent C18柱(4.6 mm×250 mm,5μm),流动相为甲醇-0.2%磷酸水(52∶48,V/V),检测波长为280 nm,以槲皮素为内标。以4 mg·kg-1的剂量给大鼠iv牛蒡苷元纳米乳,测定不同时间点的血药浓度,用DAS2.1软件计算药动学参数。结果牛蒡苷元在0.1~10 mg·L-1内线性关系良好(r=0.999 2),定量下限为0.1 mg·L-1,最低检测限为0.03 mg·L-1,提取回收率在85%以上,日内、日间RSD均小于6%。牛蒡苷元在大鼠体内的过程符合二室模型,分布半衰期和消除半衰期分别为(0.134±0.085)、(1.471±0.164)h。结论本方法可用于测定牛蒡苷元在大鼠血浆中的药物浓度,牛蒡苷元纳米乳在大鼠体内迅速分布,而且消除较慢。
OBJECTIVE To establish a HPLC method for the determination of the concentration of arctigenin in rat plasma and to study the pharmacokinetics of arctigenin nanoemulsion in rats. Methods The plasma samples were extracted with ethyl acetate. The column was Agilent C18 column (4.6 mm × 250 mm, 5 μm) with a mobile phase of methanol-0.2% phosphoric acid (52:48, V / V) To quercetin as an internal standard. At a dose of 4 mg · kg-1, rats were given iv arctigenid nanoemulsion. Blood plasma concentration was measured at different time points. Pharmacokinetic parameters were calculated by DAS2.1 software. Results Arctigenin had a good linearity (r = 0.999 2) within the range of 0.1-10 mg · L-1, the lower limit of quantification was 0.1 mg · L-1, the lowest limit of detection was 0.03 mg · L-1 and the recovery was 85 % Or more, day, day RSD were less than 6%. The process of arctigenin in rats accorded with two-compartment model. The distribution half-life and half-life were (0.134 ± 0.085) and (1.471 ± 0.164) h, respectively. Conclusion This method can be used to determine the concentration of arctigenin in rat plasma. Arctigenin nanoemulsion is rapidly distributed in rats, and its elimination is slow.