胞嘧啶的^(153)Sm标记及其用于肿瘤体内显像的可行性

The Feasibility of ^(153)Sm Labeled Cytosine in Tumor Imaging

目的探讨利用放射性核素153Sm体外标记胞嘧啶进行肿瘤代谢显像的可行性。方法胞嘧啶与DTPA的偶联产物C-DTPA,经纯化后体外标记153Sm,并对得到的显像剂C-DTPA-153Sm的质量规格进行检测:1制剂要求:检菌,热原检测;2毒理学:急性毒理测定;3特殊参数:标记率,体外稳定性;4药动学:家兔血浆药物代谢动力学;5药效学:体外细胞显像,荷瘤小鼠显像。结果体外实验、动物实验显示C-DTPA-153Sm为无菌、无热原、无毒性的安全制剂,并且可以在肿瘤部位浓集。结论 153Sm标记胞嘧啶代谢显像方法对多种肿瘤有诊断价值,可以无创性的体内评价肿瘤的增生状态,具有重要的临床应用价值。

Objective To investigate the application of153 Sm labeled cytosine in tumor metabolic imaging.Methods The cytosine was labeled with153 Sm by DTPA coupled method,the final product was C-DTPA-153 Sm.The labeled product was then purified. The determination of acute toxicity, in vitro stability, plasma pharmacokinetics in rabbits and imaging of cell and in tumor-bearing mice of radiolabeled cytosine were carried out. Results The results of examinations and animal experiments showed that the C-DTPA-153 Sm was free of bacteria,pyrogen and toxic agents,and it could be concentrated at the tumor site in tumor-bearing mice.Conclusion C-DTPA-153 Sm metabolic imaging might be used to evaluate the tumor growing status and may have important clinical value.