Ruhlmann J, Oehr P, Bender H, Kozak B, Willkomm P, Bechtold V, Lind P, Biersack H J
PET-Zentrum Bonn, Deutschland.
Acta Med Austriaca. 1998;25(1):1-6.
2-[18F]-FDG, a non-physiological glucose analogue, is the most important positron-emission- tomography (PET) radiopharmaceutical. As an example we refer to the production of 2-[18F]-FDG at the research center in Karlsruhe. 2-[18F]-FDG is synthesized in a "no carrier added" process. It is delivered at a maximal filling volume of 10 ml from a 14.5 ml batch with a batch-to-batch yield fluctuation from 5075 to 50,750 MBq and a specific activity from 1 to 10 GBq/mumol. The residual remaining synthesis reagents like solvents or catalysts have no toxicological relevance. The applicated dose per patient is in a range from 185 to 370 MBq and 1000 times lower than the correlating concentrations of stable FDG which can be regarded harmless in animals. 2-[18F]-FDG does not interfere with normal glucose metabolism. It is taken up by cells and phosphorylated to 2-[18F]-FDG-6-phosphate. The following dephosphorylation step is slow and the labeled compound is retained over several hours within the cells. Non-metabolized 2-[18F]-FDG is excreted rapidly in the urine to an extent of about 16% after 60 min, and 50% after 135 min, respectively. Fluorine-18F decays by emission of 511 KeV gamma photons. The whole body effective dose is reported to be 21 to 27 microSv/MBq. In case of an intravenous injection of 370 MBq this leads to a total dose of 7.8 to 10 mSv. The critical organ is the bladder wall (radiation dose 120 to 170 microSv/MBq or 80 to 100 mrem/mCi). The risk of a radiation induced late malignoma at 10 mSv can be estimated to be 1:2000. The genetical risk as a consequence of FDG-PET diagnostics would be 1:100,000 to 2:100,000 for dominant, and 5 times higher for recessive mutations.
2-[18F]-氟代脱氧葡萄糖（2-[18F]-FDG）是一种非生理性葡萄糖类似物，是最重要的正电子发射断层扫描（PET）放射性药物。我们以卡尔斯鲁厄研究中心生产2-[18F]-FDG为例。2-[18F]-FDG通过“无载体添加”工艺合成。它以最大填充体积10 ml从14.5 ml批次中交付，批次间产量波动范围为5075至50750 MBq，比活度为1至10 GBq/μmol。残留的合成试剂如溶剂或催化剂没有毒理学相关性。每位患者的应用剂量范围为185至370 MBq，比稳定的FDG相关浓度低1000倍，而稳定的FDG在动物体内被认为是无害的。2-[18F]-FDG不干扰正常葡萄糖代谢。它被细胞摄取并磷酸化为2-[18F]-FDG-6-磷酸。随后的去磷酸化步骤缓慢，标记化合物在细胞内保留数小时。未代谢的2-[18F]-FDG在60分钟后约16%、135分钟后50%迅速经尿液排出。氟-18F通过发射511 KeVγ光子衰变。据报道，全身有效剂量为21至27 μSv/MBq。静脉注射370 MBq时，这导致总剂量为7.8至10 mSv。关键器官是膀胱壁（辐射剂量为120至170 μSv/MBq或80至100 mrem/mCi）。10 mSv辐射诱发晚期恶性肿瘤的风险估计为1:2000。FDG-PET诊断导致的遗传风险，显性突变约为1:100,000至2:100,000,隐性突变则高5倍。
