论文部分内容阅读
目的:建立小鼠血浆中冬凌草甲素的高效液相测定方法,探讨冬凌草甲素在小鼠体内的药代动力学过程。方法:小鼠按10 mg.kg-1尾静脉注射冬凌草甲素后,不同时间点摘除眼球取血,乙酸乙酯萃取血浆,HPLC测定血浆中冬凌草甲素的浓度,并用3P97软件拟合,计算药动学参数。结果:冬凌草甲素在0.202～20.0 mg.L-1线性关系良好,r=0.998 7,测得低、中、高浓度方法回收率均大于93%,低、中、高浓度日内、日间精密度RSD均小于9%。冬凌草甲素小鼠尾静脉注射给药后,在体内呈二室模型分布,其药代动力学方程为C=16.192 5e-0.5546t+5.475 7e-0.0163t,主要药动学参数为t1/2α1.249 9 min,t1/2β42.638 4 min,K21 0.152 3 min-1,K12 0.359 3 min-1,K10 0.059 2 min-1,AUC 366.035 0μg.min-1.mL-1,CL 0.027 3 L.min-1.kg-1,VC 0.461 5 L.kg-1。结论:建立的RP-HPLC测定方法适用于体内冬凌草甲素的含量测定及药代动力学研究,冬凌草甲素在小鼠体内吸收快、分布也快,药物起效迅速,在体内以消除为主。
OBJECTIVE: To establish a method for the determination of oridonin in mouse plasma by HPLC and to study the pharmacokinetics of oridonin in mice. Methods: The mice were treated with 10 mg.kg-1 of 10 mg.kg-1 intravenous injection of oridonin at different time points, blood was removed by eyeball extraction, plasma was extracted with ethyl acetate, and the concentration of oridonin in plasma was determined by HPLC. Fit and calculate pharmacokinetic parameters. Results: The calibration curve of oridonin showed good linearity at 0.202 ~ 20.0 mg · L-1, r = 0.998 7. The recoveries of both methods were higher than 93% at low, middle and high concentrations. Inter-precision RSD is less than 9%. Oridonin intravenous injection of oridonin in mice after two-compartment model distribution, the pharmacokinetic equation C = 16.192 5e-0.5546t + 5.475 7e-0.0163t, the main pharmacokinetic parameters t1 /2α1.249 9 min, t1 / 2β42.638 4 min, K21 0.152 3 min-1, K12 0.359 3 min-1, K10 0.059 2 min-1, AUC 366.035 0 μg.min-1.mL-1, CL 0.027 3 L.min-1.kg-1, VC 0.461 5 L.kg-1. Conclusion: The established RP-HPLC method is suitable for the determination of oridonin in the body and pharmacokinetics. Oridonin absorption in mice is fast, the distribution is fast, and the drug works rapidly. In vivo To eliminate the main.