Abstract

FORMULATION AND EVALUATION OF ANTI-DIABETIC DRUGS AS CORE-IN-CUP TABLET

Radhika Parasuram Rajam*, Loganathan P., Sampathkumar Ramanathan

ABSTRACT

The present research endeavor is directed towards the development of once daily sustained release Core-in-cup tablet containing metformin hydrochloride as sustained release with pioglitazone and glimepiride as immediate release. Combination therapy concluded that Pioglitazone is effective in improving the glycemic control when added to a combination of Glimepiride and metformin in type 2 DM. Matrix system was based on the different concentrations of swellable polymer (HPMC) selected for sustaining the drug release and to get the desired release profile over a period for 12 hours. Different batches of both immediate release (IR) and Sustained release (SR) were prepared by direct compression and wet granulation method respectively. The drug-excipients incompatibility studies were performed by Fourier Transform Infrared spectrophotometer (FTIR).The granules showed satisfactory flow properties and compressibility Index. In the immediate release formulation, disintegrating agents such as sodium starch glycolate, crosspovidone were tried to get a desired release profile within 30 minutes. The in-vitro dissolution studies were performed for all the IR formulations (IR1 –IR3) and SR formulations (F1-F5). IR2 and F4 were selected for Core –in –cup tablets based on their release profile.SR formulations F4 showed release profile of 85.54% at the end of 12 hours and IR2 showed a release profile of 96.71 % of Pioglitazone and 100.68% of Glimepiride at the end of 30 minutes. Core-in-cup tablet were prepared using optimum formulation of sustained release granules (F4) and immediate release tablet (IR2). The core-in –cup tablet assay, weight variation, hardness, thickness, friability, disintegration time and in-vitro dissolution were found to be within the official limits. The dissolution data of the optimized batch was subjected to study the in-vitro release kinetics. The result showed that the IR layer of core-in cup tablet followed the first order release kinetics and the drug release kinetics of SR layer of Inlay tablet corresponds best to Higuchi‟s model and drug release mechanism as per n value of Korsmeyer & Peppas Model appeared to be a complex mechanism of swelling, diffusion and erosion with zero order release kinetics.

Keywords: Metformin Hydrochloride, Pioglitazone, Glimepiride, Core-in-Cup Tablet.