【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。更多还原

【Abstract】 Objective To investigate labeling method of [Tyr³]-octreotide with ¹²⁵I and the biodistribution of ¹²⁵I——octreotide in mice.Methods -octreotide was labeled with ¹²⁵I using the method of Chloramine-T at room temperature.NH₄HAc added to inhibit re-oxidation of ¹²⁵I——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——octreotide conformed to a two compartment open model,T_12α was 5.28 min,T_12β was 141.3 min.Conclusions The method is simple and easy to perform.The radiochemical purity is high.Labeling of ¹²⁵I——octreotide is stabile.Blood clearance of ¹²⁵I——octreotide in normal mice is quiet fast.It is excreted through gastrointestinal-liver and kidney tract.更多还原