Abstract

FORMULATION AND EVALUATION OF SUSTAINED RELEASE GASTRORETENTIVE FLOATING TABLETS OF ESOMEPRAZOLE FOR EFFECTIVE TREATMENT OF PEPTIC ULCER

Rajat Singh*, Praveen Kumar, Pratyush Jain

RKDF College of Pharmacy, SRK University, Bhopal (M.P.)

ABSTRACT

The purpose of this research was to develop a novel gastroretentive drug delivery system based on direct compression method for sustained delivery of active agent to improve the bioavailability, reduce the number of doses and to increase patient compliance for the treatment of Zollinger Ellison syndrome and peptic ulcer disease. Quick GI transit could result in incomplete drug release from the drug delivery system above the absorption zone leading to decreased efficacy of the administered dose. Gastroretentive floating tablets, which was designed to provide the desired sustained and complete release of drug for prolonged period of time. Gastroretentive floating tablets of esomeprazole were prepared by direct compression method using altered concentrations of HPMC K4, HPMC K15 as polymers. The prepared tablets of esomeprazole were evaluated for hardness, thickness, friability, weight variation, drug content uniformity, buoyancy lag time, total floating time, swelling index, in-vitro dissolution study, etc. All the compositions were resulted in adequate Pharmacopoeial limits. Compatibility studies was execution during FTIR and DSC shown that there was absence of probable chemical interaction between pure drug and excipients. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release, floating lag time and swelling index. In vitro drug release of floating gastroretentive tablet of esomeprazole shown that the formulation F6 was found to be the best formulation as it releases 99.87% esomeprazole in a controlled manner for an extended period of time (up to 12 hrs). The results indicated that a decrease in release kinetics the drug was observed increasing the polymer concentration. The release data was fitted to various mathematical models such as Higuchi, Korsmeyer-Peppas, First order and Zero order to evaluate the kinetics and mechanism of the drug release. The Optimized formulation (F6) showed no significant change in physical appearance, drug content, floating lag time, in vitro dissolution studies after 75%±5% RH at 40±20C relative humidity for 6 months. Prepared floating tablets of esomeprazole may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastroretentive drug delivery system.

Keywords: Esomeprazole, Gastroretentive, Floating tablet, Total floating time.