Preparation and characterization for multicomponent crystals of the antidiabetic drug gliquidone based on crystal engineering

Abstract

In this research, the crystal structure of antidiabetic drug gliquidone (GQD) is analysed and multicomponent crystals such as piperazine (PPZ) salt and eutectics are designed and synthesized based on its structural features. Three polymorphs of the salt are obtained together with five solvates. Fortunately, four single crystals of the salts are determined for the first time. The results reveal that the high hydrogen bond-forming ability of PPZ plays a vital role in breaking the original packing of GQD and resulting in salts instead of eutectics. Finally, comprehensive characterization of the salt polymorphs is performed and the result shows that the powder properties and powder dissolution are enhanced by the salt formation compared with the parent form.