High Solubility Crystalline Pharmaceutical Forms of Blonanserin

Abstract

Blonanserin (BLN) is an antipsychotic drug having poor aqueous solubility. In continuation of our preliminary work (CrystEngComm 2012, 14, 2367−2372), the aim of this study was to improve physicochemical properties of the drug, such as solubility, dissolution rate, and stability. Novel crystalline forms of BLN were obtained by liquid-assisted grinding with pharmaceutically acceptable coformers such as succinic acid (SUC), suberic acid (SBA), nicotinic acid (NIA), methanesulfonic acid (MSA), and toluenesulfonic acid (TsOH). Four salts of blonanerin [BLNH+–SUC– (1:1), BLNH+–NIA– (1:1), BLNH+–TsO– (1:1), and BLNH+–MSA– (1:1)], a salt hydrate BLNH+–MSA––H2O (1:1:1), and a cocrystal BLN–SBA (1:0.5) are reported in this paper. All multicomponent phases were characterized by IR, Raman, and 13C ss-NMR spectroscopy, differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD), and their structures were confirmed by single crystal X-ray diffraction. The crystal structures are sustained by ionic N+–H...