Abstract

FORMULATION AND IN VITRO, IN VIVO EVALUATION OF NATEGLINIDE-GEMFIBROZILBILAYER FLOATING BIOADHESIVE TABLETS

MD. Parveen, SK. Wajid* and Rakesh Kumar Jat

Abstract

In this research work nateglinide, gemfibrozil was selected as model drugs. Nateglinide is an amino acid derivative that induces an early insulin response to meals decreasing postprandial blood glucose levels which act by binding to β cells of the pancreas to stimulate insulin release. Gemfibrozil is used with diet changes (restriction of cholesterol and fat intake) to reduce the amount of cholesterol and triglycerides in the blood in certain people with very high triglycerides who are at risk of pancreatic disease. Formulation of sustained release floating bilayer tablets of gemfibrozil-nateglinide with HPMC K4M, Polyox WSR 303, Carbopol 971P.The compatibility of nateglinide and excipients used in study was determined using DSC and this study revealed that no interaction between drug and excipients used in the formulation. The optimized nateglinide-gemfibrozil floating formulations (NDT3, NDT9) showed satisfactory results with respect to in vitro buoyancy and sustained drug release, and was physically stable during 3 months period. The in vivo radiographic studies showed that the BaSO4-loaded floating tablets were retained in the stomach for 4.16 ± 1.57 h (n=3). The relative bioavailability of floating- tablets (NDT3) was found to be 1.7 times to that of IR tablets. This improved relative bioavailability is due to the combined effect of sustained release and increased GRT of tablets.

Keywords: Nateglinide, Gemfibrozil, floating, Natiz.