Abstract

Atorvastatin was radioiodinated and formulated using chloramine-T via an electrophilic substitution reaction for the development of a potential radiopharmaceutical for targeting liver. The impact of different reaction parameters and conditions that affected the labeling yield such as pH of the reaction, concentration of atorvastatin and reaction time were optimized in order to increase the radioiodination efficiency. The labeling yield was 94.3 ± 1.41 %. In vitro analysis demonstrated that the compound was steady for up to 24 h. The liver uptake was 40.35% and the clearance pathways proceed via the hepatobiliary and renal clearance.

中文翻译：

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阿托伐他汀的放射性碘标记为靶向肝的模型放射性药物

摘要

阿托伐他汀被放射性碘化，并通过亲电取代反应使用氯胺-T配制，以开发潜在的靶向肝的放射性药物。优化了不同反应参数和条件对标记收率的影响，例如反应的pH，阿托伐他汀的浓度和反应时间，以提高放射性碘化效率。标记产率为94.3±1.41％。体外分析表明该化合物可稳定长达24小时。肝脏吸收率为40.35％，清除途径通过肝胆和肾脏清除进行。