Development and Preparation of Controlled Release (CR) Tablet Formulations of Procainamide Fluid-Bed Technique

Abstract

The need for controlled release (CR) formulation of procainamide, an antiarrhythmic drug is well known. The aim of this investigation was an attempt to establish controlled release procainamide tablet formulations by fluid bed technique. The procainamide granules were prepared, using PVP as binder. A laboratory size fluidlzed bed drier (Uni-Glatt) was used for coating the procainamide granules. As polymers, Eudragit RSPO, ethylcelluiose and Eudragit S 100 + ethylcelluiose (1:1) have been utilized. Triethylciirate (TEC)was used as plasticizer in this investigation. The ratio of TEC to polymers was 1:9 in most experiments. However, in some formulations this ratio was increased to (1:4).
The coated granules were compressed using an excentric tabletting machine. Drug release patterns of all formulations prepared were investigated. The dissolution media were consisted of hydrochloric acid buffer pH 1.5 for the first 2h and phosphate buffer pH 8.8 for remaining period of time in all experiments.For comparison, a commercially available brand of procainamide controlled release tablet was included in this study. Cross section scanning electron micrographs of coated and uncoated granules were taken. Granules coated with Eudragit RSPO, ethylcellulose and the combination of Eudragit S 100 and ethylcellulose (1:1) exhibited proper release behaviour. The release profiles were analyzed to check whether the release was diffusion-controlled or followed first-order kinetics. The release from most of the formulations prepared seems to correspond to the first-order kinetics. It was also concluded that, air suspension technique is a suitable method for the fabrication of controlled release formulations of procainamide tablets.