Pharmaceutical cocrystals of nomegestrol acetate with superior dissolution

Abstract

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.