Evaluation of Various Grades of Hydroxypropylmethylcellulose Matrix Systems as Oral Sustained Release Drug Delivery systems

Headnote

Abstract

PURPOSE: The present work reports an attempt was to formulate matrix systems for oral sustained release drug delivery systems using diverse grades of hydroxypropyl methylcellulose (Methocel K4M, K15M, K100M and K100LV), in order to investigate the effect of various grades of these polymer on release mechanism from matrix tablets. Diclofenac Sodium was used as a model drug to evaluate its release characteristics from different matrices.

METHODS: HPMC matrix tablets of Diclofenac Sodium using HPMC (methocel K100LV K4M, K15M, K100M CR) lactose were prepared by direct compression process. The USP paddle method was selected to perform the dissolution profiles carried out by USP apparatus 2 (paddle) at 50 rpm in 900 ml 0.1 N HCl, and phosphate buffer. Drug release was analyzed according to their kinetic models. A One way analysis of variance (ANOVA) was used to interpret the result.

RESULTS: Statistically significant differences were found among the drug release profile from different matrices. At a fixed polymer level, drug release from the higher viscosity grades (K100M) was slower as compared to the lower viscosity grades (K100LV). The best-fit release kinetics was achieved with the zeroorder plot, followed by the Higuchi and Korsmeyer equations. Two formulations showed drug release is more controlled. The data obtained proved that the formulations are useful for a sustained release of Diclofenac.

CONCLUSIONS: From these formulations corresponded more controlled of the drug release by the higher viscosity grade of HPMC. The release of the model drug from these HPMC matrix tablets was prolonged; as a result, an oral release dosage form to avoid the gastrointestinal adverse effects was achieved.

Keywords: Diclofenac sodium, HPMC, Matrix tablets, Sustained Release.

(ProQuest: ... denotes formulae omitted.)

INTRODUCTION

The matrix tablet by direct compression has attracted much attention due to its technological simplicity in comparison with other controlled release systems. It required fewer unit operations, less machinery, reduced number of personnel and processing time, increased product stability and production rate [1]. HPMC, a semisynthetic derivative of cellulose, is a swellable and hydrophilic polymer. Some research groups have worked on the usage of swellable HPMC as the retarding polymer to sustain the release of different drugs [2-4]. It is very suitable to use as a retardant material in CR matrix tablets, as it is...