绿原酸在家兔体内的药动学研究

Pharmacokinetics Study On Chlorogenic Acid In Rabbits

关键词:  绿原酸  家兔  药动学

Key words:  Chlorogenic acid  Rabbit  Pharmacokinetic

摘要:

目的：本文建立了血浆中绿原酸的HPLC分析方法，比较了金银花的三种注射液中绿原酸在家兔体内的药动学差异，旨在为研究金银花连翘药对提供实验数据。方法：将18只健康无伤的家兔随机分成三组，按0.5ml?kg-1单次肌肉注射给药，用HPLC同时测定不同时间点血浆中绿原酸浓度。结果：健康家兔肌注金银花单提注射液(A)，金银花、连翘混合提取注射液（B），金银花、连翘单提合并注射液(C)后，绿原酸在家兔体内的药动学过程均符合一级吸收二室模型，绿原酸的主要药动学参数如下，A、B、C三种注射液的Cmax分别为1.567?.211mg?l-1、1.656?.143mg?l-1、1.612?.175mg?l-1；Tmax分别为0.413?.076h、0.224?.051h、0.285?.085h；Vd分别为1.895?.382L?kg-1、1.729?.413L?kg-1、1.786?.261L?kg-1；消除半衰期分别为1.164?.136h、1.227?.204h、1.132?.186h；体清除率分别为1.128?.236L?kg-1?h、0.927?.113L?kg-1?h、1.010?.142L?kg-1?h；AUC分别1.905?.303 mg?h ?L-1、2.623?.267 mg?h ?L-1、2.114?.312 mg?h ?L-1。结论：B、C注射液中绿原酸的Tmax、Tα/2、T1/2ka与A相比呈差异显著性，而Tβ/2差异不显著，表明金银花配伍连翘后，能促进绿原酸在体内吸收分布，迅速达到血峰浓度，对消除半衰期的影响不大。B与C中绿原酸的药动学参数差异不显著，表明连翘与金银花配伍时，不管是混提还是单提后合并，对绿原酸在家兔体内的药动学特征无明显影响。

Abstract:

Objective:In this article,we set up a method to analyse chlorogenic acid in plasma by HPLC, and compared the pharmacokinetic difference of chlorogenic acid in three kinds honeysuckle injection in rabbits,the objective is to analysis materia compoent of honeysuckle and forsythiae. Methods: 18 health rabbits were divided into three groups, single muscle injected with 0.5ml?kg-1, and to determine chlorogenic acid concentrations in plasma at different time points by HPLC. Results: The pharmacokinetic process of chlorogenic acid in rabbits is two-compartment model after injective the injections,the main chlorogenic acid pharmacokinetic parameters as follows,the Cmax of A、B、C is 1.567?.211mg?l-1、1.656?.143mg?l-1、1.612?.175mg?l-1;Tmax is 0.413?.076h、0.224?.051h、0.285?.085h;Vd is 1.895?.382L?kg-1、1.729?.413L?kg-1、1.786?.261L?kg-1;Eliminate half-life is 1.164?.136h、1.227?.204h、1.132?.186h;clearance is 1.128?.236L?kg-1?h、0.927?.113L?kg-1?h、1.010?.142L?kg-1?h;AUC is 1.905?.303 mg?h ?L-1、2.623?.267 mg?h ?L-1、2.114?.312 mg?h ?L-1.Conclusion: The parameter of Tmax、Tα/2、T1/2kav has significant difference between B、C and A, Tβ/2 is no significance,this show that chlorogenic acid can soon distribute in the body,the parameter of B and C has no significance,it is also show that forsythia can promote the chlorogenic acid’sabsorption and distribution in rabbit.There is no significant difference in chlorogenic acid pharmacokinetic process between B and C.