Solid-State Form Characterization of Riparin I
AbstractRiparin I is an alkamide with potential anxiolytic activity in preclinical studies. The characterization and understanding of solid-state properties play an importance role in drug development. For this work, the solid state of five riparin I batches (RIP-1, RIP-2, RIP-3, RIP-4, and RIP-5), obtained by the same synthesis process, were characterized by Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), DSC-photovisual, Thermogravimetry (TG), Fourier Transform Infrared (FTIR), Pyrolysis (Pyr-GC/MS), X-ray Powder Diffraction (PXRD), and Solid-State Nuclear Magnetic Resonance (ssNMR) techniques. Batches of riparin I with different crystal habits resulting in crystallization impurities were observed, which can be attributed to the presence of triethylamine. The main differences were observed by DSC, PXRD, and ssNMR analysis. DSC curves of RIP-2 and RIP-3 presented endothermic peaks at different temperatures of fusion, which can be attributed to the mixture of different crystalline forms. PXRD and ssNMR results confirmed crystallinity differences. The results offer evidence of the importance of controlling the reproducibility of the synthesis in order to obtain the adequate morphology for therapeutic efficacy and avoiding future problems in quality control of riparin I products. View Full-Text
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de Moura, E.A.; Terto, M.V.C.; de Moura Mendonça, E.A.; Procópio, J.V.V.; de O. Costa, V.C.; Barbosa Filho, J.M.; Chavez Gutierrez, S.J.; Tavares, J.F.; Oliveira Macedo, R.; da Silva, M.S. Solid-State Form Characterization of Riparin I. Molecules 2017, 22, 1615.
de Moura EA, Terto MVC, de Moura Mendonça EA, Procópio JVV, de O. Costa VC, Barbosa Filho JM, Chavez Gutierrez SJ, Tavares JF, Oliveira Macedo R, da Silva MS. Solid-State Form Characterization of Riparin I. Molecules. 2017; 22(10):1615.Chicago/Turabian Style
de Moura, Elisana A.; Terto, Márcio V.C.; de Moura Mendonça, Elisângela A.; Procópio, José V.V.; de O. Costa, Vicente C.; Barbosa Filho, José M.; Chavez Gutierrez, Stanley J.; Tavares, Josean F.; Oliveira Macedo, Rui; da Silva, Marcelo S. 2017. "Solid-State Form Characterization of Riparin I." Molecules 22, no. 10: 1615.
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