放射性药物化学前体间碘苄胍质量标准的建立

Establishment of Quality Standard for Metaiodobenzylguanidine as Radiopharmaceutical Precursor

  • 摘要: 间碘苄胍(MIBG)是放射性标记间碘(123I 或131I)苄胍的化学前体,为控制MIBG的质量,本研究对自制MIBG进行红外鉴别,测定溶解度、酸碱度、熔点和干燥失重等理化指标,采用ICP-MS法测定元素杂质含量,建立顶空气相色谱法测定残留溶剂无水乙醇,以及HPLC测定MIBG含量和有关物质的方法。多批次分析结果表明,自制MIBG符合人用药前体的要求,与对照品的红外图谱一致,pH在4.0~6.0范围内,熔点为167~170 ℃,干燥失重<3%,乙醇残留<0.5%,元素杂质含量低于控制阈值,MIGB有关物质未检出,MIBG含量在98.0%~102.0%范围内。本研究建立了MIBG的质量标准,可为MIBG的质量控制提供依据。

     

    Abstract: Meta-iodobenzylguanidine (MIBG) is used as a chemical precursor of radioiodinated (123I or 131I) MIBG preparation. In order to control the quality of MIBG, in this study, Infrared identification of self-made MIBG was carried out, the physical and chemical properties of solubility, pH, melting point and drying weight loss were determined, the content of elemental impurities was determined by ICP-MS, the headspace gas chromatography of residual solvent was established, and the content and related substances were determined by HPLC were established. The results for multiple batches of MIBG analysis showed that they met the requirements for medicinal precursors, the infrared spectrum of MIBG was consistent with that of the reference substance, the pH was in the range of 4.0-6.0, the melting point was 167-170 ℃, and the drying weight loss was less than 0.3%; ethanol residue was less than 0.5%, the content of elemental impurities was lower than the control threshold, together with no related impurities detected, and the contents of MIBG were 98.0%-102.0%. The quality standard of MIBG established in this study provides and provided basis for the quality control of MIBG.

     

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