Preparation, Characterization and Solubility Properties Evaluation of Pazopanib-saccharin Cocrystals

. Pazopanib (PZ) is a novel multi-target tyrosine kinase inhibitor that is currently trademarked as Votrient (R). Pazopanib-saccharin (PZ-SAC) cocrystals were prepared by mechanical ball milling, slurry crys-tallization and freeze-drying methods to improve the solubility and dissolution rate of PZ. PZ-SAC cocrystals were identified and characterized by powder X-ray diffraction, differential scanning calorimetry and Fourier transform infrared spectrometer (FTIR), and the effects of different polymers and their dosage on solubility were analyzed. Furthermore, the solubility test showed that the solubility of PZ in PZ-SAC cocrystals reached up to 2.12 mg / L compared with the solubility of pure PZ was 0.018 mg / L, the stability test also showed that PZ-SAC cocrystals had good stability. In conclusion, the PZ-SAC cocrystals particularly improved the water solubility and dissolution of PZ, which provided a theoretical basis for the development of new PZ formula-tions.