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.
[Download Article]
[Download Certifiate]