^(125)I标记的[Tyr^3]-Octreotide在小鼠体内的分布及其药代动力学研究  

The Labeling of [Tyr^3]-Octreotide with ^(125)I and Its Biodistribution and Pharmacokinetic

作　　者：朱然[1] 范我[1] 许玉杰[1] 张友九[1] 胡明江[1] 朱本兴[1] 

机构地区：[1]苏州大学放射医学与公共卫生学院江苏省放射医学与防护重点实验室,江苏苏州215007

出　　处：《苏州大学学报（医学版）》2006年第5期725-727,733,共4页Suzhou University Journal of Medical Science

基　　金：江苏省高校自然科研基金(04KJB350130);苏州大学青年教师基金(Q3126533)资助项目

摘　　要：目的探讨125I Ch-T法标记生长抑素类似物奥曲肽的方法,观察其在小鼠体内的生物学分布。方法用Ch-T法进行[Tyr3]-octreotide的125I标记,标记完成后加入NH4HAc以防止标记物的再氧化。Sephadex G-10分离纯化,纸层析测定放化纯,并行小鼠体内分布和药代实验。结果125I-[Tyr3]-octreotide比活度为5.92 TBq/mmol,标记率为76%,放化纯为95%。注射后1.0 h血液中放射性下降了90%,肠道、肝脏和肾脏中均有浓集,标记物24 h内排出体外。结论125I的Ch-T法标记[Tyr3]-octreotide放化纯高,方法简便,标记物的稳定性尚可1。25I-[Tyr3]-octreotide在小鼠体内血液清除快,药代动力学符合二室开放模型,T12α为5.28 min,T12β为141.3 min,经肠-肝途径和泌尿系统排除。Objective To investigate labeling method of [ Tyr^3 ]-octreotide with ^125I and the biodistribution of ^125 I-[ Tyr^3 ]-octreotide in mice. Methods [ Tyr^3 ]-octreotide was labeled with ^125I using the method of Chloramine-T at room temperature. NH4HAc added to inhibit re-oxidation of ^125I- [Tyr^3 ]-octreotide. The radio-chemical purity was tested with XINHUA 1 chromatography paper. Its biodistribution in normal mice was analyzed. Results The specific activity of the labeling product was 5.92TBq/mmol, The labeled yield was76 % , the radiochemical purity was 95 %. At 1. 0h after injection, radioactivity in blood decreased by 90%. Obvious accumulation of ^125I in the intestinal-liver and kidney was observed. A great amount of radioactivity was detected within 24h. The pharmacokinetic characteristics of ^125I-[Tyr^3 ]-octreotide conformed to a two compartment open model, T1/2α was 5.28 rain, T1/2β was 141.3 min. Conclusions The method is simple and easy to perform. The radiochemical purity is high. Labeling of ^125I- [ Tyr^3 ]-octreotide is stabile. Blood clearance of ^125I- [ Tyr^3 ]-octreotide in normal mice is quiet fast. It is excreted through gastrointestinal-liver and kidney tract.

关 键 词：生长抑素 碘 放射性 生物分布 药代动力学 

分 类 号：R817-33[医药卫生—影像医学与核医学]