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• W2172956404 abstract "Abstract Salt formation is a very common and effective method of improving a drug's physicochemical properties such as hygroscopicity and physical stability at different humidity conditions. Aqueous solubility is another important parameter that can be improved by salt formation; however this strategy has not yet been evaluated for the important alkaloid drug, Vinpocetine. A poorly water-soluble basic drug (water solubility value≈ 5 μg/ml and pKa value of 7.31), vinpocetine was converted into two novel salts in this work, with perchloric acid and phosphoric acid in a 1: 1 M ratio. However, an unexpected phase transformation occurred in one of the salts after the stability test, which is a major concern in studies on dosage form. The conversion of the salt to free base could be related to the temperature-humidity profile of the type II salt (formed by vinpocetine and phosphoric acid). When the temperature was more than 70 °C under high humidity conditions of more than 80%, the phase transformation occurred immediately. To gain further understanding of this phenomenon, single crystals of the two novel salts were prepared and characterized by single crystal X-ray diffraction, Powder-XRD, infrared spectroscopy, differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA). Constituents of the crystalline phase were also investigated in terms of Hirshfeld surface. The structures were found to be stabilized by H⋯H, C–H⋯O, O–H⋯N and C–H⋯π intermolecular interactions. Our stability studies showed that both these two novel salts could improve the stability of vinpocetine, however the type I salt (formed by vinpocetine and perchloric acid) offers more advantages. This finding will provide valuable information for vinpocetine dosage form development." @default.
• W2172956404 created "2016-06-24" @default.
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• W2172956404 date "2016-02-01" @default.
• W2172956404 modified "2023-10-16" @default.
• W2172956404 title "Novel perchlorate and phosphate salts of vinpocetine: Characterization, relative solid-state stability evaluation and Hirshfeld surface analysis" @default.
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• W2172956404 doi "https://doi.org/10.1016/j.molstruc.2015.10.029" @default.
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