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新型基于淀粉的肺灌注闪烁显像放射性示踪剂。

New starch-based radiotracer for lung perfusion scintigraphy.

机构信息

Inserm U646, University of Angers, 10 rue A. Boquel, 49100 Angers, France.

出版信息

Eur J Nucl Med Mol Imaging. 2010 Jan;37(1):146-55. doi: 10.1007/s00259-009-1226-6.

Abstract

PURPOSE

In order to avoid the microbiological risks linked to human serum albumin macroaggregates (MAA) used for lung perfusion scintigraphy, we developed a new starch-based Tc-99m potential radiopharmaceutical.

METHODS

Microparticles were prepared from oxidised starch coupled to natural polyamine for Tc-99m complexation. Suspensions were formulated as ready-to-use kits for easy one-step labelling procedures.

RESULTS

Particle-size analysis, electron microscopy, and confocal microscopy were performed for microparticle characterisation, and gave a typical size distribution ranging from 7 to 63 microm, with a homogenous population of spherical or oval-shaped microparticles. Radiochemical purity exceeded 95%, and was stable for at least 8 h. When challenged with histidine and human plasma, labelling was also stable. Dynamic scintigraphic acquisitions and biodistribution studies conducted on healthy Wistar rats showed a tracer accumulation with more than 80% of the ID in the lungs after 15 min.

CONCLUSIONS

With clinically significant characteristics such as a lung half-life of 3 h, a lung-to-vascular ratio of 900, and a lung-to-liver ratio of 90, starch-based microparticles exhibit all the qualities for an effective new lung perfusion agent.

摘要

目的

为避免用于肺灌注闪烁显像的人血清白蛋白大聚合体(MAA)带来的微生物学风险,我们开发了一种新型基于淀粉的 Tc-99m 潜在放射性药物。

方法

将氧化淀粉与天然多胺偶联以用于 Tc-99m 络合,制备出微颗粒。将混悬液配制成即用型试剂盒,以便于一步法标记程序。

结果

对微颗粒的特性进行了颗粒大小分析、电子显微镜和共聚焦显微镜检查,结果得到了典型的粒径分布范围为 7 至 63 微米,具有均匀的球形或椭圆形微颗粒群体。放射化学纯度超过 95%,至少稳定 8 小时。当与组氨酸和人血浆混合时,标记也稳定。在健康的 Wistar 大鼠上进行的动态闪烁采集和生物分布研究表明,在 15 分钟后,示踪剂在肺中的积累超过 ID 的 80%。

结论

基于淀粉的微颗粒具有 3 小时的肺半衰期、900 的肺血管比和 90 的肺肝比等临床显著特征,展示了作为一种有效新型肺灌注剂的所有特性。

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