Abstract

DESIGN AND CHARACTERIZATION OF SOLUBILITY ENHANCEMENT OF EZETIMIBE – A POORLY WATER SOLUBLE DRUG

Tungikar Aditya V.*, Mahale N. B. , Rode R. B. 

ABSTRACT

Poor solubility is a key factor greatly influencing their dissolution rate and bioavailability following oral administration of drugs resulting in low bioavailability. Solubility enhancement of these drugs remains one of the most challenging tasks for formulators. Hence various approaches are being explored to boost up the solubility of poorly water soluble drugs, one of such approach is using solid dispersion by fusion method. The main objective of the present study was to increase the solubility of Ezetimibe, poorly water soluble drug with low bioavailability. Ezetimibe is the first of a new class of antihyperlipidemic agents, the cholesterol absorption inhibitor, belonging to BCS class II with variable bioavailability. Soluplus was used as hydrophilic carrier. Dissolution of drug increased from all the solid dispersion. Three different formulations were prepared using Fusion Method in different ratios i.e., 1:1, 1:1.5 and 1:2 and were further characterized by FTIR, DSC, and XRD analysis. The results of FTIR revealed that no chemical interaction between the drug and the polymer exist. DSC studies showed that the drug was in amorphous state completely entrapped by the polymer. XRD studies showed the surface morphology of the solid dispersion. All the formulations showed a marked increase in drug release with the increase in the concentration of Soluplus when tested for their in-vitro studies. 1:2 ratios showed the best release with a cumulative release of 90.48% in 90 mins when compared to the pure drug. Hence, Soluplus look to be a promising carrier to improve the solubility of poorly soluble drugs.

Keywords: Solubility enhancement, Solid dispersion, Fusion method, Ezetimibe, Soluplus.