DESIGN AND OPTIMIZATION OF GASTRORETENTIVE DRUG DELIVERY SYSTEM OF SITAGLIPTIN

In the present study, Gastro retentive floating drug delivery systems (GFDDS) of sitagliptin, an anti diabetic drug, have been designed to increase the therapeutic efficacy & gastric residence time and to reduce frequency of administration. Therefore a sustained release medication was advantageous so as to achieve the prolonged therapeutic effect and to reduce peak and valley effect in plasma concentration. This can be achieved by formulating modified gastro retentive sustained release dosage forms which resides in the stomach for sufficient time to release the drug in vicinity of the absorption zone. The tablets were prepared by direct compression method, by employing polymers like HPMCK100, Poly vinyl pyrrolidine and polyacrylic acid respectively in various concentrations. The prepared granules were evaluated for angle of repose, bulk density, tapped density, compressibility index and Hausner’s ratio and results obtained were satisfactory compressed formulations were further evaluated for thickness, friability, hardness, swelling index and in-vitro dissolution studies. All the formulations showed good results which were compliance with pharmacopoeial standards. In vitro dissolution study was carried out in pH 1.2 buffers. From in vitro dissolution studies, the cumulative % drug release of all formulations ranged from 92.96% – 99.28% at the end of 12 hrs. The in vitro drug release data was fitted into various mathematical model.