Solubility enhancement of ticagrelor by co-crystal technology: Preparation, solid state characterization and solubility studies

In this study a new co-crystal of ticagrelor with quercetin has been fabricated with improved solubility. Ticagrelor is a class VI drug with poor solubility and permeability; hence an attempt has been made to improve its solubility by co-crystallization technology. A co-crystal is a structurally homogeneous crystalline material containing an active pharmaceutical ingredient and the co-former in definite stoichiometric amounts. In this study the conformer selected was quercetin based on ease of hydrogen bond formation and also as quercetin will provide a synergistic effect with ticagrelor. The co-crystal of ticagrelor with quercetin was prepared in two ratios (1:1, 2:1). Ticagrelor formed stable co-crystals in the ratios 1:1 and 2:1. The formation of co-crystal was confirmed by PXRD, DSC, and FTIR. The dynamic solubility of co-crystals in the ratios 1:1 and 2:1 increased by approximately 1.6 fold as compared to pure drug.