Formulation and Optimization of Gastroresistant Multiparticulate Drug Delivery System

Abstract

The objective of the present work was to develop a delayed release multiparticulate drug delivery system of esomeprazole magnesium trihydrate (proton pump inhibitor) to overcome the problem associated with the drug for treatment of gastric acid disorders. The formulation consisted of pellets coated with enteric coating polymer (Eudragit® L 30D 55) used for achieving a desired drug release at target site (duodenum). The core pellets composed of four different layers; seal coat, drug layer, barrier coat and enteric coat, which were optimized by altering the coating composition, concentration of coating dispersion and operating variables. The optimized formulation composed of 80% w/w coating level of Eudragit® L 30D 55 showed good acid resistant characteristics, and the % drug release in phosphate buffer pH 6.8 was found to be 99.0 ± 3.66 at the end of 15 min. Further, inadequate coating less than 80% w/w may lead to release of drug in acidic environment and excessive coating may retard the drug release. The similarity factor, f2 value was found to be 72 (≥ 50) when compared to that of marketed product. Hence it can be concluded that there is no significant difference between the dissolution profiles of formulated product with the marketed product and the developed gastro-resistant multiparticulate drug delivery system of proton pump inhibitor gave similar site specific release to the duodenum as marketed product.