Kraihammer Martin, Petřík Miloš, Rangger Christine, Gabriel Michael, Haas Hubertus, Nilica Bernhard, Virgolini Irene, Decristoforo Clemens
Department of Nuclear Medicine, Medical University Innsbruck, Anichstrasse 35, A-6020 Innsbruck, Austria.
Institute of Nuclear Medicine and Endocrinology, Kepler University Hospital, Krankenhausstrasse 9, A-4021 Linz, Austria.
Pharmaceutics. 2024 Sep 21;16(9):1231. doi: 10.3390/pharmaceutics16091231.
PET imaging of bacterial infection could potentially provide added benefits for patient care through non-invasive means. [Ga]Ga-desferrioxamine B-a radiolabelled siderophore-shows specific uptake by human-pathogenic bacteria like or and sufficient serum stability for clinical application. In this report, we present data for automated production of [Ga]Ga-desferrioxamine B on two different cassette-based synthesis modules (Modular-Lab PharmTracer and GRP 3V) utilising commercially obtainable cassettes together with a licensed Ge/Ga radionuclide generator. Quality control, including the determination of radiochemical purity, as well as a system suitability test, was set up via RP-HPLC on a C18 column. The two described production processes use an acetic acid/acetate buffer system with ascorbic acid as a radical scavenger for radiolabelling, yielding ready-to-use formulations with sufficient activity yield. Batch data analysis demonstrated radiochemical purity of >95% by RP-HPLC combined with ITLC and excellent stability up to 2 h after synthesis. Specifications for routine production were set up and validated with four masterbatches for each synthesis module. Based on this study, an academic clinical trial for imaging of bacterial infection was initiated. Both described synthesis methods enable automated production of [Ga]Ga-desferrioxamine B in-house with high reproducibility for clinical application.
细菌感染的正电子发射断层扫描（PET）成像有可能通过非侵入性手段为患者护理带来额外益处。[镓]镓去铁胺B（一种放射性标记的铁载体）对诸如[具体细菌名称1]或[具体细菌名称2]等人源致病性细菌显示出特异性摄取，并且具有足够的血清稳定性以用于临床应用。在本报告中，我们展示了利用市售试剂盒以及许可的锗/镓放射性核素发生器，在两种不同的基于试剂盒的合成模块（Modular-Lab PharmTracer和GRP 3V）上自动生产[镓]镓去铁胺B的数据。通过在C18柱上进行反相高效液相色谱（RP-HPLC）建立了质量控制，包括放射化学纯度的测定以及系统适用性测试。所描述的两种生产工艺使用乙酸/乙酸盐缓冲系统，抗坏血酸作为放射性标记的自由基清除剂，得到具有足够活性产率的即用型制剂。批次数据分析表明，通过RP-HPLC结合即时薄层色谱（ITLC），放射化学纯度>95%，并且在合成后长达2小时具有出色的稳定性。为每个合成模块建立了常规生产规范并通过四个母批次进行了验证。基于这项研究，启动了一项用于细菌感染成像的学术临床试验。所描述的两种合成方法都能够在内部自动生产[镓]镓去铁胺B，具有高度的可重复性以用于临床应用。
