Abstract

DEVELOPMENT OF RESVERATROL RAFT-FORMING CHEWABLE TABLETS WITH ACID NEUTRALIZING AND ANTI-INFLAMMATORY PROPERTIES

Kantaphon Chuaybamrung, Titayachat Mattapun, Worrawee Siripruekpong, Kanidta Kaewkroek and Ruedeekorn Wiwattanapatapee*

ABSTRACT

Raft-forming chewable tablet formulations incorporating resveratrol solid dispersion were developed to achieve prolonged drug delivery in the stomach and increase the effectiveness of gastric ulcer treatment. Solid dispersions of resveratrol in Eudragit® EPO or polyvinyl pyrrolidone K-30 were prepared first to improve the solubility of resveratrol and the optimum weight ratio of 1:7 resveratrol to Eudragit® EPO was selected to incorporate into raft-forming tablets. All tablet formulations were prepared by direct compression using sodium alginate or pectin as a gel-forming agent and hydroxypropyl methylcellulose as a release retarding polymer. Raft buoyancy was achieved by adding calcium carbonate and sodium bicarbonate as porogens. The optimized formulations formed a gelled raft in 30 sec in 0.1 N hydrochloric acid (pH 1.2) which remained buoyant and released more than 70% of resveratrol within 8 h. The formulations were capable of effective acid neutralization (6.18 mEq (Alginate#2), 8.02 mEq (Pectin#2)). Formation of a raft barrier on top of the gastric content is expected to prevent or reduce symptoms of gastroesophageal reflux disease. The formulations based on alginate and pectin exhibited potent anti-NO activity with IC50 values of 34.2 ± 0.6 μg/mL and 24.8 ± 0.4 μg/mL respectively, compared with indomethacin (14.4 ± 0.6 μg/mL).

Keywords: Raft-forming systems, Alginate, Pectin, Resveratrol, Gastric ulcers.