Formulation And Development of Delayed Release Pelletsof Proton Pump Inhibitor

Abstract

The pharmaceutical research and development mainly focus on the delivery system which is showing desired effect with minimal side effects. Multiparticulate formulations are composed of many multiple solid dosage forms administered to the mouth. This type of formulation show exponential focus on small units having optimum release profile for extended period of time. They are not only gaining dominance over the single unit dosage forms but also demonstrate good pharmacokinetic profile, dissolution rate, release profile compared to the conventional drug delivery. Multiparticulate formulation are having various benefits such as predictable gastric emptying, fast dissolution profile, increased bioavailability, less risk of dose dumping, minimum inter and intra subject variability. The aim of the present work was to develop a delayed release multi particulate drug delivery system of Drug X (Proton Pump Inhibitor) to overcome the problem associated with the gastric disorders like Peptic ulcer, Helicobacter Pylori. First of all selection of core material was done. MCC spheres were prepared using extrusion and Spheronizer. Pellets were evaluated for their flow properties, readymade sugar spheres having similar flow property with that of prepared pellets was selected for further delayed release coating. The formulation consisted of enteric coated pellets coated using enteric coating polymer (Eudragit L30D55 and combination of Eudragit L100, S100) used for achieving desired drug release at target site (Duodenum and ileum respectively). The inert pellets consist of four main layers; Drug Loading, Seal Coating, Enteric Coating and Delayed release coating which was optimized by modifying the Solid Content, Percentage coating and Process Variables. The Optimized batch is mainly consists of 25%w/w Enteric coating of Eudragit L30 D55, followed by 75% w/w Delayed release Coating of Eudragit L100 and S100 which has good acid resistance and delayed release properties. The similarity factor f2 was found to be >50 when compared to that of the innovator. Hence, it can be concluded that between marketed product and optimized batch there is no significant differences regarding dissolution profile and the developed delayed release multi particulate drug delivery system of proton pump inhibitor gave similar site specific release to the small intestine as marketed product.