Formulation and Evaluation of Floating Tablet of Coixol Showing antiulcer activity

Abstract

: Gastric ulcer is a common gastrointestinal disorder resulting from an imbalance between aggressive factors such as gastric acid, pepsin, oxidative stress, and inflammatory mediators and the protective mechanisms of the gastric mucosa. Coixol, a bioactive constituent isolated from Coix lachryma-jobi L., possesses significant antioxidant, anti-inflammatory, and gastroprotective properties; however, its therapeutic effectiveness may be limited by rapid gastric emptying and insufficient residence time at the site of action. The present study aimed to formulate and evaluate a floating gastro-retentive tablet of Coixol to enhance gastric retention and provide sustained drug release for improved anti-ulcer activity. Floating tablets were prepared by the wet granulation method using Hydroxypropyl Methylcellulose (HPMC) and Carbopol as matrix-forming polymers, while sodium bicarbonate and citric acid were incorporated as buoyancy-generating agents. The prepared formulations were evaluated for pre-compression and post-compression parameters, including flow properties, hardness, friability, weight variation, drug content uniformity, swelling behavior, floating lag time, total floating duration, and in-vitro drug release. The formulations exhibited satisfactory physicochemical characteristics, acceptable flow properties, prolonged buoyancy exceeding 12 hours, and sustained drug release profiles. Swelling studies confirmed the formation of a hydrated polymeric matrix that contributed to controlled drug release and maintenance of tablet integrity. Drug release kinetics suggested a diffusion-mediated release mechanism accompanied by polymer relaxation and matrix erosion. The findings indicate that the developed floating gastro-retentive system effectively prolongs gastric residence and sustains the release of Coixol, thereby offering a promising strategy for enhancing local drug availability and therapeutic efficacy in the management of gastric ulcer disease. Further in-vivo investigations are recommended to establish the clinical potential of the optimized formulation.