升麻素在大鼠体内的药代动力学研究

Pharmacokinetic study on cimifugin in rats

目的建立升麻素（cimifugin）血药浓度的高效液相色谱（HPLC）测定方法,研究其在大鼠体内的药代动力学特点.方法大鼠灌胃给予升麻素,取各时间点大鼠血浆,采用乙腈蛋白沉淀法,运用内标法进行HPLC检测,并用DAS2.1软件计算药代动力学参数.结果升麻素血药浓度的回归方程为Y=0.187X-0.0236,R^2=0.9982,其中升麻素在1～70mg·L^-1范围内线性关系良好,药时曲线符合二室开放模型,主要药代动力学参数Tmax、Cmax、T1/2α、T1/2z、Vd、AUC（0-t）、AUC（0-∞）分别为80min、10.359mg·L^-1、47.597min、93.131min、2.179L·kg^-1、1946.085mg·L^-1·min、2138.57mg·L^-1·min.结论建立了升麻素血药浓度方法,该方法专属性强,灵敏度高,可用于该药的体内定量分析.升麻素在大鼠体内被快速吸收达最大浓度,并发挥作用。

Aim To establish a HPLC method for de-termining cimifugin in rat plasma and investigate the pharmacokinetic characteristics of cimifugin in rats. Methods The plasma concentration of cimifugin was detected by HPLC in acetonitrile protein precipitation method after intragastric administration of cimifugin. The pharmacokinetic parameters were calculated by the procedure of DAS 2 . 1 . Results The regression equa-tion of cimifugin in rats plasma was Y =0. 187 X -0. 0236 (R2 =0. 998 2),which shows a good linear re-lation at 1 - 70 mg · L-1 . The concentration-time curves conformed to two-compartment model. The main pharmacokinetic parameters of Tmax, Cmax, T1/2α, T1/2z, Vd ,AUC(0-t) and AUC(0-∞) were 80 min, 10. 359 mg ·L-1 , 93. 131 min, 2. 179 L · kg-1 , 1946. 085 mg ·L-1 · min, 2138. 57 mg · L-1 · min, respectively. Conclusions We established a HPLC method to de-termine the concentration of cimifugin in plasma. The method is so highly specified and sensitive that it can be used in quantitative analysis in vivo on cimifugin. Cimifugin can be rapidly absorbed, reach the highest concentration and produce effect.