Modulating The Solubility of Mesalamine by Means of Cocrystals

The aim of the present research was to increase the solubility and dissolution rate of poorly water-soluble drugs through pharmaceutical cocrystal. The liquid assisted grinding method were used for the preparation of cocrystals by screening various coformers. The cocrystals were prepared in 1:1 molar ratio of drug and coformers. Initially, the resulting product was evaluated for the solubility. The selected potential cocrystal was further characterized and confirmed by FTIR, DSC, PXRD, etc. Further, dissolution rate and flowability of the selected cocrystals were also investigated. Finally, the performance of selected cocrystals was examined in the tablet dosage form. The changes in solubility provided the preliminary evidence of formation of new solid phase. In addition, the alteration in FTIR absorption, thermal behavior and PXRD pattern signaled the formation of cocrystal. Mesalamine formed cocrystal with ascorbic, sodium acetate, Urea, Saccharin Sodium and saccharin sodium showed highest solubility. The flowability of cocrystals was found superior to pure drugs. The dissolution rate of cocrystals was improved significantly as compared to original drugs. Pharmaceutical cocrystals of mesalamine having enhanced solubility, dissolution, flowability were designed, prepared and evaluated. The prepared cocrystals showed good performance in the tablet dosage form as well.