^(131)I-标记大黄素在动物体内的药物动力学和组织分布  

Pharmacokinetics and Tissue Distribution of ^(131)I-labeled Emodin Following Intravenous Administration to Animals

作　　者：杜丹[1] 吴小艾[2] 范成中[2] 梁勇[1] 辛光[1] 张瑞[1] 刘燕[1] 吴晓华[1] 何杨[1] 黄文[1] 

机构地区：[1]四川大学华西医院再生医学中心中药药理研究室&纳米生物医学技术与膜生物学研究所,四川成都610041 [2]四川大学华西医院核医学科,四川成都610041

出　　处：《应用基础与工程科学学报》2014年第1期53-57,共5页Journal of Basic Science and Engineering

基　　金：中国博士后科学基金第53批面上资助(2013M530402)

摘　　要：本文采用同位素示踪法研究尾静脉注射131I-标记大黄素在大鼠体内的药物动力学和小鼠体内的组织分布.在NBS催化剂作用下,将131I-NaI与大黄素反应得到产物2-131I-大黄素,放射性化学产率为96%,放射性化学纯度>95%,且标记物在大鼠血浆中24h内稳定.131I-标记大黄素在大鼠体内的药物动力学过程符合一室模型,半衰期(t1/2)为0.25h,清除率(CL)为0.007L/(h·kg).小鼠的组织分布特征为肺部和肾脏最高,脑组织最低,其它组织水平基本相似.研究结果表明静脉注射131I-标记大黄素后在体内分布和清除速度较快,主要经过肾脏排泄,且不易透过血脑屏障.Pharmacokinetics and tissue distribution of intravenously （ i. v. ） injected 131 I-labeled emodin in healthy rats and mice have been performed respectively by isotopic tracing method. In this study, emodin was labeled with 131 I-NaI, catalyzed by N-bromosuccinimide （NBS）, with 96% of radiolabeling efficiency and over 95 % of radiochemical purity. Meanwhile, the 2-[ 131 I ] - emodin was stable in the serum of rats during 24h. The pharmacokinetic profiles of rats after i. v. administrations, estimated by one-compartment model, revealed the half-life time （ t 1/2 ） was 15min and clearance（CL）was 0.007L/（h . kg）. The tissue distribution of mice indicated the highest amount of 131 I-labeled emodin was found in lung, followed by kidney, and the lowest was found in brain. Similar amount was shown in other tissues. The research results indicated that 131 I-labeled emodin was rapidly distributed and eliminated in the body, predominantly cleared through renal excretion, and hardly cross the blood brain barrier.

关 键 词：大黄素 药物动力学 组织分布 同位素示踪法 

分 类 号：R969.1[医药卫生—药理学]