INVESTIGATION OF THE IMPACT OF CELLULOSE ACETATE COATING ON THE RELEASE PATTERN OF FREELY SOLUBLE DRUG: METOPROLOL SUCCINATE
Keywords:
Metoprolol succinate,, cellulose acetate, controlled release tablet,, tablet coating,, pore-former,, pharmaceutical equivalence.Abstract
This study is aimed to develop and evaluate cost-effective cellulose acetate (CA)-polyvinyl pyrrolidone (PVP) film coating that can effectively control the release of freely water soluble drug, metoprolol succinate (MS) and to match that of release profile with its marketed tablet formulation. Simple core tables of MS were compressed and coated with a solution composed of semipermeable rate controlling polymer, CA and water soluble pore forming polymer, PVP. Drug-excipient interaction was investigated by both physical observation and differential scanning calorimetry (DSC). The effect of formulation parameters such as the ratio of CA to PVP, tablet coating weight gain, effect of pH on the in-vitro drug release were evaluated. Surface morphology of the CA coating membrane was examined by scanning electron microscope (SEM). Release profile of the optimized formulation at different pH conditions was determined and the similarity factor (f2) with marketed tablet release profile was calculated. It was observed that drug release rate increased with a decrease in the ratio of cellulose acetate to PVP and decreased with increased weight gain of the coating membrane. Among all the formulations, the formulation with CA and PVP at a ratio of 85:15 %w/w and 9 % weight gain showed matching release profile to the marketed tablet formulation with f2 value of 72.25. Developed MS formulation showed pH independent drug release. This study proved that CA-PVP polymer coating could effectively control the release rate of freely water soluble drugs for up to 24 h. Once a day CR formulation of metoprolol succinate pharmaceutically equivalent to marketed formulation was developed.




