花旗参在大鼠体内的药代动力学特征研究  

Harmacokinetic properties of American Ginseng in rat

作　　者：朱洪萱 黄天养 余孝云 曹永军 尚强 张存珍 余琳玲 刘连生 崔国祯 Zhu Hongxuan;Huang Tianyang;Yu Xiaoyun;Cao Yongjun;Shang Qiang;Zhang Cunzhen;Yu Linling;Liu Liansheng;Cui Guozhen(Department of Bioengineering,Zhuhai Campus of Zunyi Medical University,Zhuhai Guangdong 519041,China;National Center ofTraditional Chinese Medicine Modernization Engineering and Technological Research,Zhuhai Guangdong 519040,China;College ofPharmaceutical Sciences,Soochow University,Suzhou Jiangsu 215123,China)

机构地区：[1]遵义医科大学珠海校区生物工程系,广东珠海519041 [2]国家中药现代化工程技术研究中心,广东珠海519090 [3]苏州大学药学院,江苏苏州215123

出　　处：《遵义医科大学学报》2022年第4期438-443,共6页Journal of Zunyi Medical University

基　　金：遵义医科大学博士启动基金资助项目(NO:F-ZH-001)。

摘　　要：目的比较2种不同剂型的花旗参中皂苷Rh1、Rf、Re、Rc、Rb1在大鼠体内药代动力学主要参数,了解其在大鼠体内的变化特征与规律。方法随机将SD大鼠分为对照组、花旗参饮片组和花旗参茶组。大鼠一次性灌胃花旗参饮片提取物或者花旗参茶(75 mg/kg)后,分别在10 min~72 h内不同时间点采血。采用LC-MS法测定干预大鼠体内不同时间人参皂苷的含量变化,并采用Winnonlin软件分析主要药代动力学参数。结果大鼠口服2种不同剂型的花旗参75 mg/kg后,在大鼠血浆中检出5种成分Rh1、Rf、Re、Rc、Rb1,并分别在给药后45~60 min,60~120 min达峰。其主要药代动力学参数测定结果显示,花旗参茶组各皂苷的血药浓度时间曲线下面积(AUC_(0-t))、血药浓度峰值(C_(max))、半衰期(T_(1/2))和平均驻留时间(MRT)均大于水泡花旗参饮片组,用药以后血药浓度达到峰值所需的时间(T_(max))均小于水泡花旗参饮片组。结论口服不同剂型的花旗参在体内药代动力学参数具有明显的差别。从入血的有效成分来看,花旗参茶组在大鼠体内驻留时间和半衰期都较水泡花旗参饮片组有明显的增加,并能够在更短的时间内达到更高的血药浓度。大鼠对花旗参茶中人参皂苷的吸收、代谢明显优于水泡花旗参饮片。Objective To determine the optimal ginseng dosage form and compare the pharmacokinetics(PK)characteristics of Rh1,Rf,Re,Rc,Rb1 after single-dose oral administration of two different dosage forms of ginseng in rat.Methods SD rats were randomly divided into the control group,American ginseng water extract group,and American ginseng tea group.After single-dose oral administration of American ginseng water extract or American ginseng tea(75 mg/kg),the blood samples were collected at different time points.The ginsenoside contents,including Rh1,Rf,Re,Rc and Rb1,were measured by liquid chromatography/mass spectrometry(LC-MS),while the pharmacokinetic parameters were analyzed by Winnonlin software.Results After oral administration of American ginseng water extract or American ginseng tea(75 mg/kg),the main pharmacokinetics parameter were as follow:the measurement results of its main pharmacokinetic parameters showed that the area under the plasma concentration-time curve(AUC_(0-t)),peak plasma concentration(C_(max)),half-life(T_(1/2))and average residence time of each saponin in the American ginseng tea group(MRT)were greater than those in the group of American ginseng decoction pieces in blisters,and the time required for the blood concentration to reach the peak value(T_(max))after medication were all shorter than those in the group of decoction pieces of American ginseng in blisters.Conclusion The pharmacokinetic parameters of American ginseng in different dosage forms are significantly different in vivo.From the point of view of the active ingredients entering the blood,the residence time and half-life of the American ginseng tea group in rat are increased compared with the group of American ginseng decoction pieces in water,and it is able to reach a higher blood concentration in a shorter time.The absorption and metabolism of ginsenosides in American ginseng tea in rats are better than those in blister American ginseng pieces.

关 键 词：花旗参 药代动力学 人参皂苷 液相色谱/质谱法 

分 类 号：R961.1[医药卫生—药理学]