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Synthesis of Metforminium Succinate by Melting. Crystal Structure, Thermal, Spectroscopic and Dissolution Properties
Título:Synthesis of Metforminium Succinate by Melting. Crystal Structure, Thermal, Spectroscopic and Dissolution Properties; Synthesis of Metforminium Succinate by Melting. Crystal Structure, Thermal, Spectroscopic and Dissolution Properties
PLATA VARGAS, EDUARDO; De la Cruz Hernández, Cinthia Yareli; DORAZCO GONZALEZ, ALEJANDRO; FUENTES NORIEGA, INES; MORALES MORALES, DAVID; GERMAN ACACIO, JUAN MANUEL
The reaction by melt mixing at 220 °C of the antihypergly-cemic drug metformin hydrochloride1with dehydrated sodium suc-cinate yields efficiently the organic salt [MET]2[SUC]2(H-MET+=metforminium and SUC2-= succinate). Solid state CPMAS NMR13Cspectroscopy experiments, powder X-ray diffraction and FT-IR re-sults support the formation of the pharmaceutical salt2in goodyields. Besides, thecharged-assisted hydrogen bonding interactionsof type N-H...-O(carboxylate) were thoroughly analyzed by singlecrystal X-Ray diffraction techniques. Thus, the pharmaceutical salt2possesses considerable thermal differences when compared to thepure starting reagents. In addition, intrinsic dissolution rate expe-riments in buffered aqueous solutions at pH= 6.8 showed a sus-tained-release behavior of the drug in2with a constant value ofKint= 0.885 mg/min * cm2.