FORMULATION DEVELOPMENT AND EVALUATION OF SUSTAIN RELEASE NANOPARTICULATE TABLET OF VILDAGLIPTIN

Abstract

Vildagliptin belongs to a class of orally active anti-diabetic drug which inhibits dipeptidyl peptidase-4 (DPP-4) and to raise the emission of insulin in the β-cells, thereby decreasing blood glucose level. Current study aims to raise the dissolution rate of a water-soluble drug, Vildagliptin by the formulation of the nanoparticles. Antisolvent precipitation technique is used to manufacture Vildagliptin nanoparticles with markedly improved dissolution rate. Due to short half life, Vildagliptin is formulating into sustained release dosage form by incorporating nanoparticle system. In order to maintain the desired blood levels for an extended period of time, better drug utilization, minimum drug accumulation on chronic dosing, improved efficiency in the treatment, more uniform blood concentration, reduction in fluctuation in drug level and hence more uniform pharmacological response a sustain release formulation of Vildagliptin were designed. Vildagliptin nanoparticulate sustained release tablets was formulated using hydrophilic polymers like HPMC (K15M) and Sodium Alginate in a ratio 1:0.75 by using wet granulation method. Dissolution study done by using USP type-II dissolution apparatus gave good results with combination of HPMC K15M and Sodium Alginate. Zero order, first order, Higuchi’s equation, and Korsemeyer’s equation shows release of the drug from the formulation. The tablet formulated by using nanoparticles shows considerable increase in dissolution characteristics and bioavailability up to 98.8% which is higher than marketed formulation.