Overcoming the Drawbacks of Sulpiride by Means of New Crystal Forms

Abstract

This study aims at developing new multicomponent crystal forms of sulpiride, an antipsychotic drug. The main goal was to improve its solubility since it belongs to class IV of the BCS. Nine new adducts were obtained by combining the active pharmaceutical ingredient with acid coformers: a salt cocrystal and eight molecular salts. In addition, three novel co-drugs, of which two are molecular salts and one is a cocrystal, were also achieved. All samples were characterized in the solid state by complementary techniques (i.e., infrared spectroscopy, powder X-ray diffraction and solid-state NMR). For systems for which it was possible to obtain good-quality single crystals, the structure was solved by single crystal X-ray diffraction (SCXRD). SCXRD combined with solid-state NMR were used to evaluate the ionic or neutral character of the adducts. In vitro dissolution tests of the new crystal forms were performed and all the adducts display remarkable dissolution properties with respect to pure sulpiride.

Deep Supramolecular Language Processing for Co-crystal Prediction

“…Sulpiride experimental co-crystal screening results (× = no-co-crystal; ✓= co-crystal). The co-crystal characterization is reported in a separate pubblication [71] .…”

Thermal Stability and Kinetics of Degradation of Moxonidine as Pure Ingredient vs. Pharmaceutical Formulation

“…The stability of the drugs can be evaluated using thermoanalytical tools, which lead to crucial information on its stability under thermal stress and decomposition under different conditions (in non-isothermal and/or isothermal conditions), based on irreversible mass loss [10] and phase transitions, including polymorphic shift [11]. Additionally, in the field of pharmaceuticals, thermal analysis can provide essential data on interactions between APIs and excipients [12,13], the formation and stability of supramolecular adducts such as guest-host complexes with cyclodextrins [14][15][16][17], salts and cocrystals [18][19][20][21][22], or even semisolid formulations, such as medicated jellies [23] or gels [24].…”