Potential of RadioHPLC for the Purification of [18F]anle138b, a Candidate Radiotracer for PET Diagnostics of Parkinson’s Disease

IF 0.9 Q4 CHEMISTRY, INORGANIC & NUCLEAR
O. S. Fedorova, V. V. Orlovskaya, R. N. Krasikova
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引用次数: 0

Abstract

High radiochemical purity (RCP) is a crucial requirement to radiopharmaceuticals for positron emission tomography (PET). Semipreparative reversed-phase HPLC with UV and radioactivity detection is an efficient method for purifying radiopharmaceuticals. In separation of highly lipophilic molecules, most of the product remains on the chromatographic column owing to nonspecific sorption. We encountered this problem recently when developing a procedure for purifying [18F]anle138b, a candidate radiotracer for Parkinson’s disease diagnostics. In this study, we tested standard С18 columns, Supelco Ascentis RP-AMIDE, ACE 5 C18, and Macherey-Nagel Nucleosil, in the step gradient mode; however, the required RCP (>95%) was not reached. On the contrary, after the purification on a small monolithic Chromolith SemiPrep RP-18e column in the smooth gradient mode, RCP exceeded 98%. The procedure developed allows preparation of radiopharmaceuticals with the activity sufficient for preclinical studies.

Abstract Image

放射高效液相色谱法纯化帕金森病PET诊断候选示踪剂[18F]anle138b的潜力
高放射化学纯度(RCP)是放射性药物正电子发射断层扫描(PET)的关键要求。半制备反相高效液相色谱-紫外和放射性检测是一种有效的纯化放射性药物的方法。在分离高亲脂性分子时,由于非特异性吸附,大部分产物留在色谱柱上。我们最近在开发一种纯化[18F]anle138b的程序时遇到了这个问题,anle138b是帕金森病诊断的候选放射性示踪剂。在本研究中,我们在阶跃梯度模式下测试了标准С18色谱,Supelco Ascentis RP-AMIDE, ACE 5 C18和machery - nagel Nucleosil;然而,没有达到所需的RCP(95%)。而在小型整体Chromolith SemiPrep RP-18e柱上以光滑梯度模式纯化后,RCP超过98%。所开发的程序允许制备具有足够活性的放射性药物用于临床前研究。
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来源期刊
Radiochemistry
Radiochemistry CHEMISTRY, INORGANIC & NUCLEAR-
CiteScore
1.30
自引率
33.30%
发文量
51
期刊介绍: Radiochemistry  is a journal that covers the theoretical and applied aspects of radiochemistry, including basic nuclear physical properties of radionuclides; chemistry of radioactive elements and their compounds; the occurrence and behavior of natural and artificial radionuclides in the environment; nuclear fuel cycle; radiochemical analysis methods and devices; production and isolation of radionuclides, synthesis of labeled compounds, new applications of radioactive tracers; radiochemical aspects of nuclear medicine; radiation chemistry and after-effects of nuclear transformations.
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