原儿茶酸在大鼠体内的药动学及组织分布  

Pharmacokinetics and tissue distribution of protocatechuic acid in rats

作　　者：杨丽丽[1] 汪电雷[1,2] 陶秀华[1] 曹银[3] 汪辰吟[1] 陈金佩[1] 

机构地区：[1]安徽中医药大学,安徽合肥230038 [2]安徽中医药大学药物代谢动力学研究室 [3]安徽省合肥市精神病医院,安徽合肥230038

出　　处：《中国医院药学杂志》2014年第4期263-266,共4页Chinese Journal of Hospital Pharmacy

基　　金：国家自然科学基金资助项目(编号:81001592);教育部科学技术重点项目(编号:210101);安徽高校省级自然科学研究重点项目资助(编号:KJ2010A210;KJ2012A186)

摘　　要：目的:建立HPLC法测定大鼠血浆和组织中的原儿茶酸,并研究其在大鼠体内的药动学及组织分布特征。方法:单剂量灌胃给予大鼠12.5,25,50 mg·kg-1的原儿茶酸,用HPLC法测定各时间点的血药浓度并用DAS 2.0软件处理数据。大鼠灌胃给药25 mg·kg-1,测定给药10,30,60 min后主要组织中的原儿茶酸浓度。结果:原儿茶酸在大鼠体内药动学符合二室开放模型,主要药动学参数:原儿茶酸的Cmax分别为(0.34±0.06),(1.59±0.07),(3.03±0.34)mg·L-1。AUC(0-t)分别为(38.97±4.35),(147.53±17.35),(423.64±61.58)mg·min·L-1。组织分布结果表明,原儿茶酸主要分布于胃、肾、心脏,其次分布于肝、肌肉和脾,脑和肺分布较少。结论:所建立的HPLC法样品前处理简便、操作简便、能满足原儿茶酸在大鼠体内的药动学及组织分布研究。OBJECTIVE To establish a HPLC method for the determination of protocatechuic acid （PA） in rat plasma and tissue. METHODS A single oral dose of PA was performed in rats at 12. 5, 25, 50 mg kg-1 , plasma concentrations at each time point were determined by HPLC and the data were analyzed by DAS 2. 0. The concentrations of PA in the main tissues were determined at 10, 30 and 60rain after an oral administration of 25 mg kg-1. RESULTS The pharmacokinetics of PA con- formed to a two compartment open model after ig administration. The main pharmacokinetic parameters were Cmax （mg. L-1 ） ： 0. 34 ± 0. 06,1.59 ± 0. 07,3. 03 ± 0. 34; AUC（0-t） （mg. min. L-1 ） ： 38. 97 ± 4. 35,147. 53 ± 17. 35,423. 64 ± 61.58. PA was main- ly distributed in stomach, kidney, heart, less in liver, muscle and spleen,and least in brain and lung. CONCLUNION A sim- ple, rapid, accurate and precise HPLC method for the analysis of PA in rat plasma was successfully developed and validated and successfully applied to a pharmacokinetic and tissue study of PA in rats.

关 键 词：原儿茶酸 高效液相色谱法 药动学 组织分布 

分 类 号：R969.1[医药卫生—药理学]