Abstract

STOMACH SPECIFIC GASTRORETENTIVE FLOATING TABLET OF ANTI-HYPERLIPIDEMIC DRUG: FORMULATION DEVELOPMENT AND IN-VITRO CHARACTERIZATION

*Kapoor D, Patel M, Vyas RB, Chaitali Lad, Sharma S

ABSTRACT

The aim of the present study to develop the various processing parameters and formulations aspects for developing a pharmaceutical equivalent, stable, cost improved and quality improved formulation of floating tablet of Simvastatin comparable with innovator and optimize certain process parameters to get maximum yield of the product during large scale manufacturing. Being a Class II drug, Simvastatin shows slow dissolution rate, limited oral absorption and high variability in pharmacological effects. Gastro retentive floating tablet of Simvastatin was prepared by direct compression technique using HPMC K15M as the rate controlling polymer. The hydrophilic cellulose derivative, HPMC K15M was evaluated for its gel forming and release controlling properties. Sodium bicarbonate and citric acid were incorporated as gas generating agents. The effects of soluble components (sodium bicarbonate and citric acid) and gel forming agents on drug release profile and floating properties were investigated. The tablets from all formulations were evaluated for thickness, diameter, weight variation, hardness, and friability. In vitro drug release, kinetic data and related stability studies after optimization of promising formulation of selected drug are being done to exhibit diffusion dominant drug release and its stability may be attributed to that the present problem certainly will be helpful and surely will open an avenue for new trend of control drug delivery system. The release mechanisms were explored and explained with zero order, first order, Higuchi, Hixon Crowell and Korsmeyer equations. The release rate, extent and mechanisms were found to be governed by the polymer content. It was found that the mean dissolution time, percentage drug release, release rate constant and diffusion exponent were influenced significantly by the amount of polymer incorporation.

Keywords: Floating, Simvastatin, HPMC K15M, Sustained rlelease, in-vitro release studies.