Tang Xiaolan, Tang Ganghua, Nie Dahong
College of Science, Southern China Agricultural University, Guangzhou 510642, China.
Appl Radiat Isot. 2013 Dec;82:81-6. doi: 10.1016/j.apradiso.2013.07.012. Epub 2013 Jul 26.
Automated synthesis of (11)C-acetate ((11)C-AC) as the most commonly used radioactive fatty acid tracer is performed by a simple, rapid, and modified solid-phase extraction (SPE) purification.
Automated synthesis of (11)C-AC was implemented by carboxylation reaction of MeMgBr on a polyethylene Teflon loop ring with (11)C-CO2, followed by acidic hydrolysis with acid and SCX cartridge, and purification on SCX, AG11A8 and C18 SPE cartridges using a commercially available (11)C-tracer synthesizer. Quality control test and animals positron emission tomography (PET) imaging were also carried out.
A high and reproducible decay-uncorrected radiochemical yield of (41.0 ± 4.6)% (n=10) was obtained from (11)C-CO2 within the whole synthesis time about 8 min. The radiochemical purity of (11)C-AC was over 95% by high-performance liquid chromatography (HPLC) analysis. Quality control test and PET imaging showed that (11)C-AC injection produced by the simple SPE procedure was safe and efficient, and was in agreement with the current Chinese radiopharmaceutical quality control guidelines.
The novel, simple, and rapid method is readily adapted to the fully automated synthesis of (11)C-AC on several existing commercial synthesis module. The method can be used routinely to produce (11)C-AC for preclinical and clinical studies with PET imaging.
作为最常用的放射性脂肪酸示踪剂,(11)C-乙酸盐((11)C-AC)的自动化合成通过简单、快速且经过改进的固相萃取(SPE)纯化来进行。
(11)C-AC的自动化合成通过在聚四氟乙烯环上用甲基溴化镁与(11)C-二氧化碳进行羧化反应来实现,随后用酸和强阳离子交换柱进行酸性水解,并使用市售的(11)C-示踪剂合成仪在强阳离子交换柱、AG11A8和C18固相萃取柱上进行纯化。还进行了质量控制测试和动物正电子发射断层扫描(PET)成像。
在约8分钟的整个合成时间内,从(11)C-二氧化碳获得了高且可重复的未校正衰变放射性化学产率(41.0±4.6)%(n = 10)。通过高效液相色谱(HPLC)分析,(11)C-AC的放射性化学纯度超过95%。质量控制测试和PET成像表明,通过简单的固相萃取程序制备的(11)C-AC注射是安全有效的,并且符合现行中国放射性药物质量控制指南。
这种新颖、简单且快速的方法很容易适用于在几种现有的商业合成模块上对(11)C-AC进行全自动合成。该方法可常规用于制备用于PET成像的临床前和临床研究的(11)C-AC。