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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: To study the pharmacokinetics and tissue distribution of isocorynoxeine in rats. Methods: After administration of 40, 80 mg / kg rhynchophylline respectively, the drug concentration in plasma and tissues and organs of rats were determined by HPLC and the drug was calculated by DAS2.0 software non-compartment model parameter estimation Dynamic parameters. Results: The main pharmacokinetic parameters were as follows: T max 0.5,0.25 h, C max 0.07,0.29 mg / L and T 1/2 ) Were 1.01 and 1.09 h respectively, the AUC_ (0-t) values were 0.08,0.31 mg / (L · h), CL were 499.33 and 235.27 L / (h · kg), MRT_ (0 -∞) , 1.59h, Vd respectively 732.82,369.20L / kg. According to a single dose of 80mg / kg single dose, the different rhynchophylline in each tissue are distributed in the gastrointestinal tract in the highest mass fraction, the lowest brain. Conclusion: The established method is rapid, accurate and easy to meet the requirements of pharmacokinetics study of Rhynchophylline.