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奥曲肽类似物68Ga DOTA NOC的放射性标记、质量控制及放射化学纯度评估

Radiolabelling, quality control and radiochemical purity assessment of the Octreotide analogue 68Ga DOTA NOC.

作者信息

Di Pierro D, Rizzello A, Cicoria G, Lodi F, Marengo M, Pancaldi D, Trespidi S, Boschi S

机构信息

PET Radiopharmacy-Nuclear Medicine, Azienda Ospedaliero, Universitaria di Bologna, S. Orsolo-Malpighi Hospital, Via Massarenti 9, 40318 Bologna, Italy.

出版信息

Appl Radiat Isot. 2008 Aug;66(8):1091-6. doi: 10.1016/j.apradiso.2007.12.001. Epub 2007 Dec 8.

Abstract

Somatostatin receptors 1-5 are over expressed in neuroendocrine tumours (NETs). 68Ga-labelled [1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid]-1-Nal3-Octreotide (DOTA NOC), a recent synthesized somatostatin analogue, shows high affinity for those receptors. Herein, modifications of a commercial module for the labelling of DOTA NOC with 68Ga, as well as the assessment of time course of the radiochemical purity variation are described. The evaluation of radiochemical stability was done by two different chromatographic methods: reversed-phase radio HPLC and fast TLC analysis. Labelled compound has been found radiochemically stable within 3h from the end of labelling (EOL) and radiochemical purity was always higher than 99%. After 73 labelling sessions the system showed great reproducibility and high radiochemical yield.

摘要

生长抑素受体1 - 5在神经内分泌肿瘤(NETs)中过度表达。68Ga标记的[1,4,7,10 - 四氮杂环十二烷 - 1,4,7,10 - 四乙酸]-1 - Nal3 - 奥曲肽(DOTA NOC),一种最近合成的生长抑素类似物,对这些受体显示出高亲和力。本文描述了用于用68Ga标记DOTA NOC的商业模块的改进,以及放射化学纯度变化的时间进程评估。通过两种不同的色谱方法进行放射化学稳定性评估:反相放射性高效液相色谱法和快速薄层色谱分析。已发现标记化合物在标记结束(EOL)后3小时内放射化学稳定,放射化学纯度始终高于99%。经过73次标记实验后,该系统显示出高度的重现性和高放射化学产率。

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