Abstract

DESIGN AND OPTIMIZATION OF EXTENDED RELEASE TABLETS OF VILDAGLIPTIN BY MATRIX DIFFUSION SYSTEM USING DIRECTLY COMPRESSIBLE CO-PROCESSED EXCIPIENTS.

Ammar Ashraf Awan*, Nazar M Ranjha and Umar Farooq

ABSTRACT

Vildagliptin is an anti diabetic agent that provides the glycemic control to patients of Type 2 diabetes. The normal dose for Vildagliptin is either 50 mg or 100 mg each day. The dose of 50 mg is to be taken once a day, while the dose of 100 mg is taken as a divided doses of 50 mg twice a day. In market Vildagliptin is available as the dosage form of tablets. Tablets can be prepared by direct compression as well as wet granulation method. The aim of this research work was to develop a directly compressible controlled release polymer by co- processing the two polymers i.e; Xanthum gum (natural polymer) & Eudragit L 100 (synthetic polymer) by solvent evaporation method and then use that co-processed polymer to formulate extended release matrix tablets of Vildagliptin by direct compression method. In co-processing the interaction occurs at sub particle level between two or more excipients which results in granulation that have better flow properties than the individual excipients. Co-processing alters the physico-chemical properties of individual excipients. Co-processing also helps in reducing the tendency of capping, prevents storage of elastic energy during compression and reduces lamination. Coprocessing has the benefits of improved flow properties, improved compressibility, better dilution potential and improvement in binding and blending properties. In the present study an extended release matrix tablet was prepared exhibiting good sustained drug release for a time period of 8 hours. Trial formulation T7 had 35% of co processed excepients with a ratio of 1:1 between Xanthan gum & Eudragit L 100. This could be helpful to lower the dosing frequency of Vildagliptin from twice a day to once a day.

Keywords: Vildagliptin, Co-processed polymers, extended release matrix tablet, Type 2 Diabetes mellitus, Xanthan gum, Eudragit L 100.