Abstract

FORMULATION AND EVALUATION OF AGOMELATINE SUBLINGUAL TABLETS EMPLOYING ITS SOLID DISPERSIONS

K. Santosh Kumar*, V Murali Manoj and T R Ranjini

ABSTRACT

The objective of the current investigation is to formulate and evaluate agomelatine sublingual tablets employing its solid dispersions. Agomelatine belongs to class II under BCS and exhibits low and variable oral bioavailability due to its poor aqueous solubility and higher first-pass metabolism. As such it needs enhancement in the dissolution rate and bypass of first-pass metabolism in its formulation development to derive maximum therapeutic efficacy. Preparation of solid dispersion is one of the successful techniques for solubility enhancement of insoluble drugs. The compatibility of agomelatine with PVP K30 was confirmed by FTIR spectroscopy. The solid dispersions were prepared by solvent evaporation method, using methanol as common solvent, and were analysed for drug content uniformity and dissolution rate study. The solid dispersions that showed better dissolution rate was selected for formulation into tablets. The SD3 solid dispersions of the drug to polymer ration 1:3 were selected for tablet formulation. Agomelatine sublingual tablets were prepared by direct compression method using two different super disintegrants CCS and SSG at three different concentrations 2%, 3% and 4% individually. The prepared tablets were evaluated for physicochemical characteristics and invitro dissolution rate studies. Different kinetic parameters were calculated for the evaluation of prepared tablets. Agomelatine dissolution from prepared tablets was rapid and higher in all formulations and it followed first order kinetics. The tablets formulated employing CCS showed better dissolution rate compared to those formulated with SSG and the dissolution rate of agomelatine increases with the concentration of particular superdisintegrant due to decrease in disintegration time, which makes the drug readily available for dissolution. Among all the formulations, the formulation F6 containing 4% CCS showed better results with respect to dissolution parameters, so it was concluded that F6 is the optimised formulation for the preparation of agomelatine sublingual tablets.

Keywords: Agomelatine, Solid Dispersions, Solubility enhancement, Dissolution efficiency.