Modafinil Cocrystals for Altered Physicochemical Properties

The present investigation was designed to prepare and characterize BCS class II drug modafinil cocrystals for its solubility enhancement and other properties. Hansen solubility parameter (HSP) was used for prediction of cocrystal formation. Coformers/excipients namely boric acid, cinnamic acid, salicylic acid, and tartaric acid were used in the preparation of cocrystals by liquid assisted grinding method with 1:1 molar ratio of drug and coformer. The prepared cocrystals were subjected to characterization by performing melting point determination, solubility analysis at its saturation point, and drug release by in vitro method. Furthermore, characterization was also done by Fourier Transform IR spectroscopy, Differential Scanning Calorimetry, PXRD and Scanning Electron Microscopy. The formation of modafinil cocrystals by using cinnamic acid and salicylic acid and the formation of modafinil complexes with boric acid and tartaric acid were confirmed by collectively assessing the results. Moreover, a drastic improvement in the solubility revealed the importance of preparing pharmaceutically useful cocrystals of marketed active pharmaceutical ingredients (APIs). However, the increased dissolution rates were seen with cocrystals but not with the complexes. Thus solid state manipulation technique can be used to improve the physicochemical properties of an API using HSP as a successful tool for the prediction of cocrystal formation among the partners.