Pharmaceutical cocrystals of nomegestrol acetate with superior dissolution

The improvement of solubility and dissolution properties are the focus of research on poorly water-soluble APIs. Cocrystallization, which offers a different approach to modify properties of APIs, has gained considerable interest recently. Herein, we designed and synthesized two novel nomegestrol acetate (NA) cocrystals using 2,5-dihydroxybenzoic acid (DA) and 4-hydroxybenzoic acid (PA). Both cocrystals were characterized by single-crystal X-ray diffractometry (SCXRD), powder X-ray diffractometry (PXRD), Fourier transform infrared spectroscopy (FT-IR), and differential scanning calorimetry (DSC). Powder dissolution studies indicated that the concentrations of NA-DA and NA-PA at 3 h are approximately 5 and 4 times that of NA in deionized water, respectively. These successful results imply that the cocrystallization strategy is an effective means to improve the solubility of NA. The improvement of solubility and dissolution properties are the focus of research on poorly water-soluble APIs.