An ultrasonographic assisted investigation for the enhancement of duodenal/cecal motility of mosapride through a surfactant-based triple solid dispersion: In-vitro, in-vivo assessment of tablet formulation

Abstract Gastrointestinal (GI) disorders affect millions of people and are considered a major cause of global morbidity. Mosapride citrate (MOS) is a prokinetic agent with antiemetic effect. The drug suffers from poor bioavailability that is induced by its low solubility. The present study aimed to enhance the in-vivo performance of the drug through formulation of fast release tablets. Both binary (SD) and triple solid dispersion (TSD) were prepared with Soluplus® (SOL) and α-Tocopherol polyethylene glycol succinate (TPGs) using solvent evaporation. Optimal systems were chosen according to the best dissolution rate and were compressed into tablets using either, AcDiSol, Crospovidone, or chitosan as superdisintegrants. Results declared that MOS-TSD acquired the highest dissolution rate in terms of t1/2 = 1.5 min. DSC and XRPD illustrated a partial amorphization of mosapride. FTIR revealed a possible H bond interaction between drug and carriers. Drug release from MOS-TSD tablets containing Crospovidone showed 60.7% flush release with a t1/2 = 1.4 min. An ultrasonographic study performed on rabbits revealed that MOS-TSD tablet with optimum carrier combination showed 2.46 -fold increase in duodenal and cecal motility compared to pure MOS and 2.5-fold increase compared to the oral marketed product. Therefore, the formulation of fast release tablet with surfactant based triple solid dispersion offered a great success in improving the therapeutic efficacy of mosapride.