检索历史 清除

摘要Objectives The objectives of this study were to prepare and characterize the novel myricetin cocrystals and to demonstrate the enhanced solubility and dissolution.Methods The experiments based on the solution method yielded four cocrystals, with nicotinamide (NIC), isonicotinamide (INM), caffeine (CAF), 4-cyanopyridine (CYA) and reaction crystallization experiments were carried out to scale-up the hits.Solid-state characterization was carried out by PXRD, DSC, IR spectroscopy and liquid-state NMR analysis.Solubility and dissolution studies were performed by comparison with its pure components in different pH buffers.Phase transition was showed through the creation of a ternary phase diagram.Key findings Four new solid myricetin cocrystals with unique melting point, DSC, FTIR and PXRD data was obtained.The molar ratio of four cocrystals was different: MYR-CAF (1∶1),MYR-CYA (1∶3), MYR-NIC (1∶2), MYR-INM (1∶2).The cocrystals had a pH-independent dissolution profile and showed a nearly ten-fold increase in the dissolution efficiency in different pH buffers.The crystal structures of four cocrystals were solved by single-crystal X-ray diffraction and were analyzed in terms of their supramolecular synthons.