Formulation And In Vitro, In-Vivo Evaluation Of Floating Bi Layer Tablets Of Ezetimibe- Nateglinide

Abstract

In this research work, nateglinide, ezetimibe were 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. Ezetimibe is a lipid-lowering compound
that inhibits intestinal cholesterol and phytosterol absorption. Formulation of sustained release floating bilayer
tablets of ezetimibe-nateglinide with Polyox WSR 303, Carbopol 934P, HPMC K4M, Na CMC. 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-ezetimibe floating
formulations (NGT3, NGT10) 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).