Abstract

SOLUBILITY ENHANCEMENT AND PHYSICOCHEMICAL CHARACTERIZATION OF TADALAFIL BY INCLUSION COMPLEXATION METHOD

Swapnila V. Shinde*, Farheen Shaikh and Anuja N. Gawande

ABSTRACT

In the present research work Tadalafil (TDF) used as a model drug. It is an antihypertensive drug belongs to BCS class II drug. It’s poor water solubility i. e 3.48 μg/ml makes a suitable drug candidate for solubility enhancement. For the solubility enhancement combination of hydrophilic carriers and hydroxyl acids such as β-cyclodextrin, Hydroxy propyl-β-cyclodextrin, Citric acid and Tartaric acid were used respectively. In the preliminary study physical mixtures of TDF were prepared using hydrophilic carriers and hydroxyl acids. Based on the solubility results for further preparation of inclusion complexes combination of β-CD and Citric acid were used. Inclusion complexation (IC) were prepared by kneading and solvent evaporation method. Prepared complexes were then characterized physicochemically for saturation solubility study, XRD, DSC, SEM and CDR. The study results shown inclusion complex prepared by kneading method shown marked improvement in the solubility as compared to solvent evaporation method. Further inclusion complex prepared by kneading method were used to formulate conventional tablet. The prepared tablet were evaluated for pre compression and post compression study. IC containing conventional tablet then compared with marketed formulation for drug release study and shown significant improvement in the drug release from IC-conventional tablet as compared to marketed tablet. Inclusion complex prepared by kneading method and conventional tablet was found to be stable in stability study.

Keywords: Tadalafil, Inclusion Complexation, ?-cyclodextrin, Citric acid, Conventional tablet.