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A Novel Method for the Synthesis of 99mTc-Ofloxacin Kits Using D-Penicillamine as Coligand and Their Application as Infection Imaging Agent

机译:D-青霉胺为配体合成99mTc-氧氟沙星试剂盒的新方法及其作为感染显像剂的应用

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摘要

The employment of radiopharmaceuticals is increasing nowadays for infection imaging and early execution of patients having infectious or inflammatory complaints. The main aim of this study was to discover a novel method for the labeling of ofloxacin with 99mTc, optimization of labelling conditions to get higher percent yield, to assess kits radiochemical purity, in vitro stability, partition coefficient, protein binding, and intracellular accumulation in Pseudomonas aeruginosa, Salmonella typhi, and Escherichia coli in infected rabbits. Maximum labeling efficiency was achieved when 1.5 mg ofloxacin was labeled with 10–20 mCi sodium pertechnetate in the presence of 3 mg D-penicillamine, 75 μg SnCl2. In vitro binding and biodistribution in Pseudomonas aeruginosa, Salmonella typhi, and Escherichia coli showed good results. This new complex is efficient for the imaging of infections caused by Gram-positive and Gram-negative bacteria.
机译:如今,对于感染成像和感染性或炎症性疾病患者的早期治疗,放射性药物的使用正在增加。这项研究的主要目的是发现一种用 99m Tc标记氧氟沙星的新方法,优化标记条件以获得更高的产率,以评估试剂盒的放射化学纯度,体外稳定性,分配系数感染兔中的铜绿假单胞菌,伤寒沙门氏菌和大肠杆菌中的蛋白,蛋白结合和细胞内积累。在3μmgD-青霉胺,75μgSnCl2存在的情况下,用10–20μmCi高net酸钠标记1.5μmg氧氟沙星可以达到最大的标记效率。在铜绿假单胞菌,伤寒沙门氏菌和大肠杆菌中的体外结合和生物分布显示了良好的结果。这种新的复合物可有效用于对革兰氏阳性和革兰氏阴性细菌引起的感染进行成像。

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