Formulation and Evaluation of Extended Release Floating Matrix Tablet of Eperisone Hydrochloride by Direct Compression Method

摘要

Increased complications and costs of marketing of innovative drugs focused greater attention to the development of sustained release (SR) or controlled release (CR) drug delivery systems. Delivery systems extended release or controlled release rate can achieve predictable and reproducible, the extended duration of activity for the short time of life - drugs, reduced toxicity and dose reduction request, the optimized therapy and better patient compliance. It is controlled primarily by the type and the proportion of the polymers used in the preparation. Eperisone hydrochloride is a centrally acting muscle relaxant acting through poly and mono-synaptic reflexes in the spinal cord, exhibits vasodilator effect, increases blood flow and inhibits the pain reflex pathway. The objective of present work was to develop and evaluated oral extended release floating matrix tablet of eperisone HCl prepared by the method of direct compression, using hydroxy propyl methyl cellulose (HPMC K15, HPMC K4) and PVP K30 as matrix formation polymers. Sodium bicarbonate and citric acid was used as gas generating agents. The FTIR spectra of the eperisone HCl and other excipients alone and in combination show the compatibility of the drug and excipients. Nine formulations of different polymer percentages were formulated (F1-F9). Pre-compression parameters were evaluated. The influence of matrix forming agents and binary mixtures of them on eperisone HCl release was investigated. The formulated tablets were characterized by thickness and diameter, drug content, hardness, friability, uniformity of weight, In vitro buoyancy studies and dissolution rate studies. The formulated tablets had acceptable physicochemical characters. The data obtained from the in-vitro dissolution studies of optimized batch F7 were fitted in different models. The optimized formulation F7 showed 99.45±0.45% drug content and floating lag times of 65±4 sec. Drug release mechanism was found to be first order kinetics. Eperisone HCl floating tablets exhibited increased gastric residence time, there by improved bioavailability and therapeutic effect of the drug.