^(11)C-胆碱合成模块小型化及其应用

Miniaturization of the ^(11)C-choline synthesis module and its application

目的 11C-胆碱是与18F-FDG互补的PET/CT肿瘤显像剂,使用设备合成该药需要涉及11C-胆碱/蛋氨酸合成模块(PET-CS-Ⅰ)、11C-碘代甲烷/乙酸盐合成模块(PET-CS-Ⅱ)以及活度仪,共计3台设备,占用2个合成热室。为提高热室利用率,该研究将PET-CS-Ⅰ进行了小型化改造。方法首先用AutoCAD布局作图,选择一个新的小型箱体,经铣、钻等工艺后,将原模块内的部件安装至新箱体,同时缩短内部管线并最优化安置各电子器件,防止相互干扰。然后按原设备合成原理、反应步骤、所需试剂合成11C-胆碱,质量控制体系不变。再分别进行安全性和生物分布实验,荷W250大鼠和人前列腺癌PET/CT显像。结果改造后的新模块仅22 cm×18 cm×13 cm大小,体积缩小80%,可与其他11C药物合成模块及活度计放在一起,只占用1个热室。所合成的11C-胆碱用高效液相色谱(HPLC)检验时无碘代甲烷,放化纯度为99%,化学收率达90%以上。使用安全,生物分布同文献报道,能被W250活性肿瘤组织摄取,显示人前列腺癌原发灶及其转移灶优于18F-FDG。结论改造后的11C-胆碱模块体积明显缩小,合成效率和药物质量不变,可有效用于前列腺癌的诊断与分期。

Objective 11C-choline is a type of tumor tracer used as a complement to 18F-FDG.Its synthesis required three devices including 11C-choline/methionine integration module(PET-CS-Ⅰ),11C-iodomethane/acetate integration module(PETCS-Ⅱ) and dose calibrator,taking up two hot cells.This study focused on dwindling the PET-CS-Ⅰto improve the utilization of the hot cells.Methods First of all,the primary equipment parts were measured and drawn by using AutoCAD,then a new compact cab was chosen.The units in the original were fixed into the new cab.The internal lines and locations of the electronic devices were optimized.After 11C-choline was synthesized,the quality control system was remained unchanged.A biodistribution study in normal SD rats,PET/CT scan of the W250 tumor-bearing SD rats and prostate cancer patients were done.Results The new 11Ccholine/methionine integration module was 22 cm×18 cm×13 cm,and the volume decreased about 80% compared to the original one.No iodomethane was detected in 11C-choline synthesis by the new module,examined by HPLC.The radiochemical purity was over 99%.There were different biodistributions from 18F-FDG,high radioactive uptake in tumor and good T/NT ratio.Conclusion The new module showes a smaller volume and a raised synthetic efficiency.11C-choline we produced is with high quality and capable to use for diagnosis and staging of prostate cancer.