Pretze Marc, Wendrich Jan, Hartmann Holger, Freudenberg Robert, Bundschuh Ralph A, Kotzerke Jörg, Michler Enrico
Department of Nuclear Medicine, University Hospital Carl Gustav Carus, Technical University Dresden, Fetscherstr. 74, 01307 Dresden, Germany.
Eckert & Ziegler Eurotope, 13125 Berlin, Germany.
Pharmaceuticals (Basel). 2024 Dec 28;18(1):26. doi: 10.3390/ph18010026.
(1) : Targeted alpha therapy is an emerging field in nuclear medicine driven by two advantages: overcoming resistance in cancer-suffering patients to beta therapies and the practical application of lower activities of Pb- and Ac-labelled peptides to achieve the same doses compared to beta therapy due to the highly cytotoxic nature of alpha particles. However, quality control of the Pb/Ac-radiopharmaceuticals remains a challenge due to the low activity levels used for therapy (100 kBq/kg) and the formation of several free daughter nuclides immediately after the formulation of patient doses; (2) : The routine alpha detection on thin-layer chromatograms (TLC) of Pb- and Ac-labelled peptides using a MiniScanPRO+ scanner combined with an alpha detector head was compared with detection using an AR-2000 scanner equipped with an open proportional counter tube. Measurement time, resolution and validity were compared for both scanners; (3) : For Ac, the quality control values of the radiochemical purity (RCP) were within the acceptance criteria 2 h after TLC development, regardless of when the TLC probe was taken. That is, if the TLC probe was taken 24 h after radiosynthesis, the true value of the RCP was not measured until 5 h after TLC development. For Pb-labelled peptides, the probe sampling did not have a high impact on the value of the RCP for the MiniScanPRO+ and AR-2000. A difference was observed when measuring TLC with the AR-2000 in different modes; (4) : The MiniScanPRO+ is fast, does not require additional equipment and can also measure the gamma spectrum, which may be important for some radiopharmaceutical production sites and regulatory authorities. The AR-2000 has a better signal-to-noise ratio, and this eliminates the need for additional waiting time after TLC development.
(1):靶向α治疗是核医学中一个新兴领域,其得益于两个优势:克服癌症患者对β治疗的耐药性,以及由于α粒子具有高度细胞毒性,可实际应用较低活度的铅和锕标记肽来达到与β治疗相同的剂量。然而,由于治疗所用活度水平较低(100 kBq/kg)以及在制备患者剂量后立即形成多种游离子核素,铅/锕放射性药物的质量控制仍然是一项挑战;(2):将使用MiniScanPRO+扫描仪结合α探测器头对铅和锕标记肽的薄层色谱图(TLC)进行常规α检测,与使用配备开放式正比计数管的AR - 2000扫描仪进行检测相比较。对两台扫描仪的测量时间、分辨率和有效性进行了比较;(3):对于锕,无论何时采集TLC探针,放射化学纯度(RCP)的质量控制值在TLC展开后2小时内均在验收标准范围内。也就是说,如果在放射性合成后24小时采集TLC探针,直到TLC展开后5小时才测量到RCP的真实值。对于铅标记肽,探针采样对MiniScanPRO+和AR - 2000的RCP值影响不大。使用AR - 2000在不同模式下测量TLC时观察到了差异;(4):MiniScanPRO+速度快,不需要额外设备,还能测量γ能谱,这对一些放射性药物生产场所和监管机构可能很重要。AR - 2000具有更好的信噪比,这消除了TLC展开后额外的等待时间。