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利用99m锝-葡庚糖酸盐(99mTc-GHA)通过转螯合作用制备99m锝-乙二半胱氨酸(99mTc-EC)及其在肾功能研究中的评估。

Preparation of 99mTc-ethylene dicysteine (99mTc-EC) by transchelation using 99mTc-glucoheptonate (99mTc-GHA) and its evaluation for renal function studies.

作者信息

Vanaja R, Solav S V, Joshi S H, Kumar P, Ramamoorthy N

机构信息

Radiopharmaceuticals Programme, Board of Radiation and Isotope Technology (BRIT), BARC Vashi Complex, Navi, Mumbai, India.

出版信息

Nucl Med Commun. 2000 Oct;21(10):977-82. doi: 10.1097/00006231-200010000-00014.

Abstract

The complexation of ethylene dicysteine (EC) with 99mTc needs to be carried out at pH 12 to achieve a high radiochemical yield. However, the preparation of the kit at high pH poses difficulties and requires very stringent preparation conditions, as stannous tin, one of the main ingredients in the kit, is unstable at high pH. Hence, an alternative method, involving the transchelation preparation of 99mTc-EC using 99mTc-glucoheptonate (99mTc-GHA) prepared at pH 6.5, was attempted, prompted by the reported success of the preparation of 99mTc-sestamibi (99mTc-MIBI) by this method. The preparation of 99mTc-EC by this method first involved the formation of 99mTc-GHA by the addition of sodium pertechnetate-99mTc to the Sn-GHA kit vial at pH 6.5. 99mTc-EC was formed by the addition of reconstituted EC solution at pH approximately 12 to the preformed 99mTc-GHA. The reaction was allowed to proceed both at room temperature and on a boiling water bath. The pH of the final product was adjusted to pH approximately 7 with 0.5 M phosphate buffer at pH 4-5, without affecting the quality of the product. The urinary excretion of 99mTc-EC prepared by transchelation, tested in mice, was similar to that of directly prepared 99mTc-EC, indicating that the final product prepared by the two methods was the same. The clinical evaluation of the product formulated by the new procedure showed satisfactory findings, comparable with the reports in the literature.

摘要

乙烯二半胱氨酸(EC)与99mTc的络合需要在pH 12的条件下进行,以获得较高的放射化学产率。然而,在高pH值下制备试剂盒存在困难,并且需要非常严格的制备条件,因为试剂盒中的主要成分之一亚锡在高pH值下不稳定。因此,受通过这种方法成功制备99mTc-司他莫比(99mTc-MIBI)报道的启发,尝试了一种替代方法,即使用在pH 6.5制备的99mTc-葡庚糖酸盐(99mTc-GHA)进行99mTc-EC的转螯合制备。通过这种方法制备99mTc-EC首先涉及在pH 6.5下将高锝酸钠-99mTc添加到Sn-GHA试剂盒小瓶中形成99mTc-GHA。通过将pH约为12的重构EC溶液添加到预先形成的99mTc-GHA中来形成99mTc-EC。反应在室温下和沸水浴中进行。用pH 4-5的0.5 M磷酸盐缓冲液将最终产物的pH调节至约pH 7,而不影响产物质量。在小鼠中测试的通过转螯合制备的99mTc-EC的尿排泄与直接制备的99mTc-EC相似,表明两种方法制备的最终产物相同。通过新程序配制的产品的临床评估显示出令人满意的结果,与文献报道相当。

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