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  • Synthesis of Metforminium S...
    Plata-Vargas, Eduardo; De la Cruz-Hernández, Cinthia; Dorazco-González, Alejandro; Fuentes-Noriega, Inés; Morales-Morales, David; Germán-Acacio, Juan Manuel

    Journal of the Mexican Chemical Society, 10/2017, Letnik: 61, Številka: 3
    Journal Article

    The reaction by melt mixing at 220 °C of the antihyperglycemic drug metformin hydrochloride 1 with dehydrated sodium succinate yields efficiently the organic salt MET2SUC 2 (H-MET+= metforminium and SUC2- = succinate). Solid state CPMAS NMR 13C spectroscopy experiments, powder X-ray diffraction and FT-IR results support the formation of the pharmaceutical salt 2 in good yields. Besides, the charged-assisted hydrogen bonding interactions of type N-H…-O(carboxylate) were thoroughly analyzed by single crystal X-Ray diffraction techniques. Thus, the pharmaceutical salt 2 possesses considerable thermal differences when compared to the pure starting reagents. In addition, intrinsic dissolution rate experiments in buffered aqueous solutions at pH= 6.8 showed a sustained-release behavior of the drug in 2 with a constant value of Kint = 0.885 mg/min * cm2.