七叶胆苷ⅩⅤⅡ大鼠体内药代动力学研究  

Pharmacokinetics of gypenoside ⅩⅤⅡ in rats

作　　者：王超[1,2] 顾冬冬[2] 王彦[2] 韩雪春[1] WANG Chao GU Dong-dong WANG Yan HAN Xue-chun(Tongrea Hospital Affiliated to School of Medicine, Shanghai Jiaotong University, Shanghai 200336, China School of Pharmacy, Shanghai Jiaotong University, Shanghai 200240, China)

机构地区：[1]上海交通大学医学院附属同仁医院,上海200336 [2]上海交通大学药学院,上海200240

出　　处：《中国中药杂志》2017年第4期783-788,共6页China Journal of Chinese Materia Medica

摘　　要：应用高效液相色谱-质谱联用分析方法,建立七叶胆苷ⅩⅤⅡ体内分析方法,方法学结果显示线性范围为1~2 500μg·L^(-1)(r=0.996 3);高、中、低3种不同浓度的日内RSD分别为9.9%,3.0%,1.7%;日间RSD分别为16%,14%,2.5%;基质效应90.0%~100%,RSD<15%;回收率>80.0%。对大鼠静脉和灌胃给予七叶胆苷ⅩⅤⅡ对照品后测定血浆中浓度随时间的动态变化过程,绘制药时曲线,并根据药时曲线计算药代动力学参数。用DAS 2.0软件计算得到七叶胆苷ⅩⅤⅡ在大鼠体内口服药代动力学参数t_(max)为0.17~0.20 h,t_(1/2)为1.94~2.56 h,生物利用度为1.87%。结果显示七叶胆苷ⅩⅤⅡ药动学特征为口服吸收分布快,达峰时间快,消除快。In this study,we established an HPLC-MS method to determine gypenoside ⅩⅤⅡ in biosamples. The methodology results indicated that the linear range was 1-2 500 μg·L^（-1）（ r = 0. 996 3）; intraday RSD values for high,medium and low concentrations were 9. 9%,3. 0% 1. 7%; interday RSD values were 16%,14%,2. 5%; matrix effect ranged between 90. 0%-100%,with RSD 15%. The recovery was more than 80. 0%,with precision and accuracy in line with request. After the rats were orally and intravenously administered with gypenoside ⅩⅤⅡ,the concentrations of gypenoside ⅩⅤⅡ in plasma were determined,and pharmacokinetic parameter was calculated using pharmacokinetic software DAS 2. 0. According to the main pharmacokinetic parameters of gypenosideⅩⅤⅡ,t（max） was 0. 17-0. 20 h,t（1/2）was 1. 94-2. 56 h,bioavailability of oral administration was 1. 87%. The results indicated that the pharmacokinetic profiles of gypenoside ⅩⅤⅡ were rapid absorption and distribution after oral administration,short time to peak and rapid elimination.

关 键 词：七叶胆苷ⅩⅤⅡ 药代动力学 LC-MS/MS 血药浓度 

分 类 号：R285.5[医药卫生—中药学]