Recent Approach on Determination of Impurities and Degradation Products/Causes for m-Iodobenzylguanidine Using HPLC-Tandem Mass Spectrometry | Chapter 1 | Current Advances in Chemistry and Biochemistry Vol. 3

 m-Iodobenzylguanidine hemisulfate  (MIBGHS) is a precursor for radioiodine-labeled m-iodobenzylguanidine (MIBG), which is used as a radio-imaging and therapy agent for neuroendocrine tumours and myocardial sympathetic nerve activity. The purity of the precursor, source of impurity, and derivatives must all be calculated in order to ensure the medicine's consistency and effectiveness while avoiding side effects. The purity of synthesised MIBGHS and the amount of contaminants found in it were calculated using high-performance liquid chromatography and ultraviolet detection on both C8 and phenyl type columns, with gradient eluted by ammonium formate aqueous solution and acetonitrile mobile phase. Process-related impurities such as m-bromobenzylguanidine (MBrBG) and overreacted byproducts were discovered, according to the findings. MIBGHS is stable for at least 72 hours under acidic and dry thermal conditions, but MIBG aqueous solution decomposes slowly when exposed to UV light, thermal, oxidative, and alkaline environments, according to stress test results. As a result, the starting material for the synthesis of MIBGHS, m-iodobenzylamine, should be analysed to ensure that it is free of m-bromobenzylamine impurity. MIBGHS is stable for at least 12 months when stored at room temperature (-18°C). MIBGHS is unstable due to the chemically labile guanidine and amine groups, with iodide loss from the phenyl group being a minor cause. Both pollutants, derivatives, and degenerates derived from the reaction activity of the guanidine or amine groups, as well as the MIBG's weak phenyl-iodine bond, are non-toxic at normal therapeutic doses, but they can reduce the effective dose of radioiodine-labeled MIBG.

Author(s) Details

Dr. Wei-Hsi Chen
Chemistry Division, Institute of Nuclear Energy Research, Taoyuan City, Taiwan, ROC.

Yu Chang
Chemistry Division, Institute of Nuclear Energy Research, Taoyuan City, Taiwan, ROC.

Ching-Yun Lee
Chemistry Division, Institute of Nuclear Energy Research, Taoyuan City, Taiwan, ROC.

Shiu-Wen Liu
Chemistry Division, Institute of Nuclear Energy Research, Taoyuan City, Taiwan, ROC.
 
Wen-Ching Wu
Chemistry Division, Institute of Nuclear Energy Research, Taoyuan City, Taiwan, ROC.

Tsai-Yueh Luo
Technology Promotion Center, Institute of Nuclear Energy Research, Taoyuan City, Taiwan, ROC.

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