试剂盒制剂活性药物成分d,l-HMPAO作为脑灌注诊断系统

M. Davarpanah, H. Abbasi, M. Nabati, Hamideh Sabahnoo, Vida Bodaghi-Namileh, M. Mazidi, Hossein Movahhed-Tazehkand, Hossein Mohammadnejad-Mehrabani
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引用次数: 3

摘要

本研究的目的是制备用于99m-锝放射性核素标记的Exametazime (d,l-HMPAO)试剂盒作为脑灌注诊断系统。第一步分两步制备活性药物成分d - l-HMPAO,纯度为99.29%;采用元素分析、傅里叶变换红外光谱(FT-IR)和核磁共振(NMR)技术对其分子结构进行了表征。第二步,用六种不同的配方制备d,l-HMPAO试剂盒,并用锝-99m放射性核素标记。高放射化学产率归因于高SnCl2量和磷酸盐缓冲液的加入。动物实验是在3个月大的雄性Wistar大鼠身上进行的。生物分布研究表明,所有大鼠的平均脑活度均在1% ID/g以上。结果表明,合成的化合物(d,l-HMPAO)具有较高的同分异构纯度,并对建议的配方进行了优化。
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Kit formulation of active pharmaceutical ingredient d,l-HMPAO as a brain perfusion diagnostic system
The purpose of this research study is to prepare Exametazime (d,l-HMPAO) kit for labeling with 99m-technetium radionuclide as a brain perfusion diagnostic system. In first step, the active pharmaceutical ingredient d,l-HMPAO was prepared in two steps with the purity of 99.29 %. Its molecular structure was characterized using elemental analysis, Fourier-transform infrared spectroscopy (FT-IR) and nuclear magnetic resonance (NMR) technique. In second step, the d,l-HMPAO kit was prepared using six different formulations and labeled by technetium-99m radionuclide. The high radiochemical yield was attributed to the high amount of SnCl2 and adding phosphate buffer. The animal studies were conducted on three-month old male Wistar rats. The biodistribution studies revealed that, the mean activity in brain of all rats was above 1% ID/g. This showed the high isomerism purity of the synthesized compound (d,l-HMPAO) and optimization of the suggested formulations.
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