摘要
目的:研究异去氢钩藤碱(Isocorynoxeine)在大鼠体内的药代动力学及组织分布特征。方法:大鼠灌胃分别给予40、80mg/kg的钩藤总碱后,采用HPLC法检测血浆和组织器官中各时间点的药物浓度,并用DAS2.0软件非房室模型参数估算法计算药动学参数。结果:分别给予40、80mg/kg钩藤总碱后主要药动学参数如下:T_(max)分别为0.5、0.25h,C_(max)分别为0.07、0.29mg/L,T_(1/2)分别为1.01、1.09h,AUC_(0-t)分别为0.08、0.31mg/(L·h),CL分别为499.33、235.27L/(h·kg),MRT_(0-∞)分别为1.43、1.59h,Vd分别为732.82、369.20L/kg。按80mg/kg单剂量单次给药后,异去氢钩藤碱在各组织中均有分布,在胃肠道中的质量分数最高,脑中最低。结论:所建立的方法快速、准确、简便,能够满足异去氢钩藤碱的药动学研究要求。
Objective：Objective To study the pharmacokinetics and tissue distribution of isocorynoxeine in rats.Methods：The plasma and tissue concentration of isocorynoxeine were detected by HPLC method after intragastric administration of 40,80mg/kg total alkaloids.The pharmacokinetics was calculated according to non-compartment model by the procedure of DAS2.0.Results：The absorption was fast after intraduodenal administration of The total alkaloids of Uncaria（40mg/kg,80mg/kg）to rats with Tmax of 0.5h and 0.25 h,Cmax of 0.07 and 0.29mg/L,T1/2） of 1.01 and 1.09 h,AUC0-t of 0.08 and 0.31mg/（L·h）,CL of 499.33 and 235.27L/（h·kg）,MRT0-∞ of 1.43 and 1.59 h,Vd of 732.82 and 369.20L/kg,respectively.Isocorynoxeine was distributed widely after oral administration dose of 80mg/kg in rat,and highest content in the gastrointestinal tract,lowest in brain.Conclusion：The developed method is rapid,accurate and simple,and can satisfy the requirement of pharmacokinetic study of isocorynoxeine in rat.
出处
《亚太传统医药》
2016年第1期18-21,共4页
Asia-Pacific Traditional Medicine
基金
贵州省剑河中药材产业科技合作计划项目(剑科合字[2014]4号)
