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利用从基于SnO₂的⁶⁸Ge/⁶⁸Ga发生器洗脱的⁶⁸Ga对DOTATATE进行放大放射性标记。

Scaled-up radiolabelling of DOTATATE with 68Ga eluted from a SnO2-based 68Ge/68Ga generator.

作者信息

Rossouw Daniel D, Breeman Wouter A P

机构信息

Radionuclide Production Department, iThemba LABS, PO Box 722, 7129 Somerset West, South Africa.

出版信息

Appl Radiat Isot. 2012 Jan;70(1):171-5. doi: 10.1016/j.apradiso.2011.07.016. Epub 2011 Jul 28.

Abstract

A scaled-up radiolabelling and improved post-labelling purification procedure for [(68)Ga]DOTATATE is reported, using a more than 1 year old SnO(2)-based 1850MBq (68)Ge/(68)Ga generator (initially double-loaded with 3700MBq (68)Ge) as a source of ionic (68)Ga. The elution method of choice comprised elution with 0.6M HCl in a single 4mL fraction, containing up to 95% of the total eluted (68)Ga activity. The unpurified fraction was directly used for labelling after pH adjustment with 2.5M sodium acetate. Labelling efficiencies were determined at 90-95°C at various reaction times and reaction volumes of up to 5.7mL, using either 30μg or 50μg DOTATATE. Only the latter amount resulted in consistently high labelling efficiency in excess of 95%. Post-labelling purification, carried out on Sep-Pak C18, showed that 50% ethanol in saline was a superior desorption eluant than 100% ethanol. The highest and most consistent decay-corrected radiochemical yields (89%) were obtained using 50μg DOTATATE and a 20min reaction time.

摘要

报道了一种用于[(68)Ga] DOTATATE的放大放射性标记和改进的标记后纯化程序,使用了一台超过1年的基于SnO(2)的1850MBq(68)Ge/(68)Ga发生器(最初双装载3700MBq(68)Ge)作为离子(68)Ga的来源。选择的洗脱方法包括用0.6M HCl在单个4mL馏分中洗脱,该馏分含有高达95%的总洗脱(68)Ga活度。未纯化的馏分在用2.5M醋酸钠调节pH后直接用于标记。在90-95°C下,在不同反应时间和高达5.7mL的反应体积下,使用30μg或50μg DOTATATE测定标记效率。只有后一种用量导致始终高于95%的高标记效率。在Sep-Pak C18上进行的标记后纯化表明,盐水中50%的乙醇是比100%乙醇更好的解吸洗脱剂。使用50μg DOTATATE和20分钟反应时间获得了最高且最一致的衰变校正放射化学产率(89%)。

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