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通过选择性沉淀从 Sr 中简便地放射化学分离临床级 Y,用于靶向放射性核素治疗。

Facile radiochemical separation of clinical-grade Y from Sr by selective precipitation for targeted radionuclide therapy.

机构信息

Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai 400 085, India; Homi Bhabha National Institute, Anushaktinagar, Mumbai 400 094, India.

Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai 400 085, India; Homi Bhabha National Institute, Anushaktinagar, Mumbai 400 094, India.

出版信息

Nucl Med Biol. 2019 Jan-Feb;68-69:58-65. doi: 10.1016/j.nucmedbio.2019.01.002. Epub 2019 Jan 19.

Abstract

INTRODUCTION

The widespread clinical utilization of Y for preparation of target specific radiopharmaceuticals demands development of a facile, efficient and cost-effective method for radiochemical separation of Y from Sr viaSr/Y generator. In this article, we describe an efficient and facile method for radiochemical separation of Y from Sr for preparation of radiopharmaceuticals by exploiting the large difference in the solubility product constants (K) of Y(OH) and Sr(OH).

METHODS

A two-step radiochemical separation procedure based on selective precipitation of Y under alkaline conditions from Sr/Y equilibrium mixture was developed. The Y(OH) colloid formed at pH ~ 10 was selectively trapped in 0.22 μm sterile filter and was subsequently retrieved by dissolution in HCl solution. Detailed quality control analyses of obtained Y were carried out and its utility towards preparation of different radiopharmaceuticals was assessed.

RESULTS

Using the same feed solution of Sr (3.7 GBq), consistent and repeated separation of Y could be achieved in different batches with >85% yield and >99.999% radionuclidic purity. Yttrium-90 obtained from this process was found suitable for preparation of therapeutically relevant doses of three different radiopharmaceutical formulations, namely, Y-DOTA-TATE, Y-PSMA-617 and Y-CHX-A″-DTPA-Cetuximab with >95% radiochemical purity.

CONCLUSIONS

The promising results obtained in this study would facilitate implementation of the developed technique for obtaining Y in adequate quantity and of required purity from a centralized radiopharmacy setup.

摘要

简介

由于 Y 广泛应用于靶向放射性药物的制备,因此需要开发一种简便、高效且经济有效的方法,以便通过 Sr/Y 发生器从 Sr 中分离出 Y 进行放射性化学分离。本文描述了一种从 Sr 中分离 Y 以制备放射性药物的高效、简便方法,该方法利用 Y(OH)和 Sr(OH)的溶度积常数(K)之间的巨大差异。

方法

基于从 Sr/Y 平衡混合物中在碱性条件下选择性沉淀 Y 的两步放射性化学分离程序。在 pH 值为~10 时形成的 Y(OH)胶体被选择性地截留在 0.22 µm 无菌过滤器中,并随后用 HCl 溶液溶解回收。对获得的 Y 进行了详细的质量控制分析,并评估了其在制备不同放射性药物中的应用。

结果

使用相同的 Sr 进料溶液(3.7GBq),可以在不同批次中以>85%的产率和>99.999%的放射性核纯度反复实现 Y 的一致分离。从该过程获得的 Y-90 适合用于制备三种不同放射性药物制剂的治疗相关剂量,即 Y-DOTA-TATE、Y-PSMA-617 和 Y-CHX-A″-DTPA-Cetuximab,其放射性化学纯度均>95%。

结论

本研究中获得的有前途的结果将有助于从集中式放射性药物制剂中以足够的数量和所需的纯度获得 Y 的开发技术的实施。

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