Oxaliplatin-flavone pharmaceutical co-crystal-CN111205332A: patent spotlight

Co-crystallization is a technique for modifying physicochemical properties of pharmaceutical ingredients with an aim to enhance the therapeutic efficacy and subsequent reduction in toxicity. The patent describes the development of oxaliplatin co-crystals using flavonoids (baicalein and naringenin) via solvent volatilization technique with an objective to improve solubility and stability in GI tract and reduced side/toxic effects. The co-crystals were characterized via differential scanning calorimetry, thermogravimetric analysis, x-ray diffraction analysis. The co-crystals exhibited slow drug release, delayed hydrolysis, low cytotoxicity and enhanced therapeutic activity on human gastric adenocarcinoma cells. However, suitable solvent for co-crystal production, large scale production and regulatory challenges for continuous manufacturing of co-crystals must be addressed.