Research on Rebamipide Sustained-release Tablets Using Solubilization Technology and Gastric Retention System

Rebamipide is a widely used drug for patients with gastrointestinal mucosal lesions that require long-term treatment. It has a narrow absorption zone in the upper small intestine and exhibits reduced solubility at low pH. Since the upper small intestine has a relatively low pH environment due to the influence of the gastrointestinal tract, the current method of administering rebamipide is not optimal. Therefore, this study aimed to develop an optimal formulation that improves solubility at low pH by applying solubilization technology and increases the retention time in the upper small intestine, the main absorption site, using a gastric-retentive sustained-release formulation. In previous research, a solid dispersion with improved solubility at low pH was prepared. In this study, the prepared solid dispersion was combined with sodium bicarbonate and sustained-release agents. Specifically, a gastric-retentive sustained-release tablet was developed that improves dissolution at low pH and allows for controlled sustained-release patterns through a combination of hydroxypropyl methylcellulose and carrageenan. In conclusion, this study confirmed the potential value of a new formulation that can optimize the therapeutic effect of rebamipide.