SOLUBILITY ENHANCEMENT OF AMISULPRIDE BY SOLID DISPERSION TECHNIQUE AND PREPARATION OF FAST DISSOLVING TABLETS

Amisulpride exhibits anti-psychotic activities by selectively binding to
dopamine D(2) and D(3) receptors in the limbic system. It is used in the
treatment of psychoses, paranoid, productive schizophrenias, dysthymia.
However, amisulpride (AMP) is poorly water soluble drug, so solubility is
the main constraint for oral bioavailability. An attempt has been made to
increase the solubility of this drug by formulating solid dispersion (SD) by
using β-cyclodextrin (β-CD) employing spray drying method and then
formulating fast dissolving tablets(FDT). Among the two different
formulation of SD, formulation SD2 containing amisulpride & β-CD in the
ratio of 1:2 gives best drug content and dissolution profile and among tablet
formulations. FDTs were prepared by direct compression technique using
superdisintegrants such as croscarmellose sodium and sodium starch
glycolate in different concentrations. SDs were characterized by FT-IR,
DSC analysis and evaluated for drug content and in vitro dissolution
profiles. Tablet formulations were evaluated for pre compressional
parameters such as angle of repose, bulk & tap density, Carr’s index,
Hausner’s ratio and post compression parameters such as hardness,
friability, weight variations, drug content, wetting time, disintegration time
and in vitro dissolution profile. Formulation CF2 containing 6.5%
croscarmellose sodium gives best disintegration and dissolution profile
compared with other formulations. Results showed that β-cyclodextrin is a
promising polymer for enhancing the solubility of AMP