胡黄连苦苷Ⅰ大鼠药动学及血浆蛋白结合率研究

Pharmacokinetics of picroside Ⅰ in rats in vivo and determination of plasma protein binding rate

建立大鼠血浆中胡黄连苦苷Ⅰ的HPLC-UV测定方法,研究在大鼠体内的药代动力学特征,同时测定其血浆蛋白结合率.血浆样品经乙腈沉淀蛋白后,上清液直接进样测定.采用Diamonsil((钻石)C18色谱柱(4.6 mm×250 mm,5μm)流动相为甲醇∶水∶醋酸(45∶55∶0.1),检测波长282 nm,流速1 mL/min,采用3p97药动学软件对药时数据进行拟合.结果表明大鼠尾静脉注射胡黄连苦苷Ⅰ符合二室开放模型,胡黄连苦苷Ⅰ在大鼠体内分布代谢很快,消除较快.

To establish a HPLC-UV method for determining picroside Ⅰ in rat plasma and study pharmacokinetics characteristic in rat in vivo,determine plasma protein binding rate.The supernatant was determined directly after the protein in plasma sample was precipitated by acetonitrile.Dikma Diamonsil C18 was seleted,methanol-water-acetic acid mixture was used as mobile phase,the detective wavelength at 282 nm,the flow rate at 1.0 mL/min.The concentration-time data were processed by 3p97 pharmacokinetics software.PicrosideⅠcan be fitted to two-compartment model after iv administrated.Picroside Ⅰ was distributed and metabolism quickly and eliminated soon.