欧前胡素在大鼠体内的药动学与组织分布研究  

Study on Pharmacokinetics and Tissue Distribution of Imperatorin in Rats

作　　者：张笑恺[1] 曹蔚[1] 谢艳华[1] 段林瑞[1] 王四旺[1] 

机构地区：[1]第四军医大学药学系药物研究所,西安710032

出　　处：《中国药房》2013年第3期216-219,共4页China Pharmacy

摘　　要：目的:建立欧前胡素在生物样品中的分析测定方法,并进行欧前胡素在大鼠体内药动学和组织分布研究。方法:采用液-液萃取方法进行生物样品预处理;采用高效液相色谱法测定大鼠灌胃欧前胡素后不同时间的血药浓度。色谱柱为HypersilBDSC18(250mm×4.6mm,5μm),流动相为乙腈-水(60:40,V/V),流速为1.0ml/min,柱温为25℃,内标为异欧前胡素,检测波长为300nm。以DAS2.0版药动学程序软件计算药动学参数,并进行组织分布研究。结果:血浆和组织样品中欧前胡素和异欧前胡素峰面积比值与欧前胡素血药浓度在一定范围内线性关系良好(r≥0.9984);样品加样回收率均在87.69%以上,日内、日间精密度的RSD为0.58%～6.15%和0.53%～8.00%,稳定性的RSD为0.56%～6.99%。大鼠口服欧前胡素后体内代谢符合二室模型(W=1),tmax=2.5h,cmax=(1.45±0.49)mg/L,AUC0-∞=(7.03±2.27)mg(/h.L);并在组织中广泛分布。结论:本方法简便、快捷、灵敏、准确,适用于欧前胡素的药动学和组织分布研究。OBJECTIVE：To establish the method for the determination of imperatorin in biological samples,and to study the pharmacokinetics and tissue distribution of imperatorin in rats.METHODS：The analytes were prepared by a liquid-liquid extraction method.Rats were given imperatorin,blood concentration of tamoxifen was determined by HPLC-UV.The separation was performed on Hypersil BDS C 18（250 mm×4.6 mm,5 μm）using acetonitrile-water（60：40,V/V）as mobile phase at flow rate of 1.0 ml/min.The column temperature and ultraviolet detection were performed at 25 ℃ and 300 nm.Isoimperatorin was used as the internal stand.The data were calculated by DAS2.0 software.The tissue distribution of imperatorin were studied.RESULTS：Good linear calibration curves for the plasma and tissues were obtained（r≥0.998 4）,and the recovery was greater than 87.69% for each sample.The intra-day and inter-day RSDs were 0.58%-6.15% and 0.53%-8.00%,and RSDs of stability were 0.56%-6.99%.The concentration-time curve of imperatorin in rat plasma could be fitted to two-compartment model（W=1）,t max =2.5 h,c max =（1.45±0.49）mg/L,AUC 0-∞ =（7.03±2.27）mg（/h.L）;and imperatorin was widespread in tissues.CONCLUSION：The method is simple,rapid,sensitive and accurate,and is suitable for pharmacokinetics and tissue distribution study of imperatorin in plasma and tissues of rats.

关 键 词：欧前胡素 白芷 高效液相色谱法 药动学 组织分布 

分 类 号：R285[医药卫生—中药学] R969.1[医药卫生—中医学]