Abstract
Objective: The present study focused on solubility enhancement of the Biopharmaceutical Classification System (BCS) Class-II drug, Febuxostat using various super disintegrants.
 Methods: Starches were extracted from Entada scandens seed powder by alkali method i.e., sodium hydroxide at 0.1%, 0.25% and 0.5% concentrations and water. Starches were evaluated for various phytochemical and physicochemical tests. Solid dispersions of Febuxostat were prepared by fusion method using poloxamer-188 alone and by mixing poloxamer-188 with Entada scandens seed starch. Various physical parameters were evaluated for these solid dispersions. Tablets were prepared using Febuxostat solid dispersions and varying concentrations of Entada scandens seed starch by direct compression technique. Pre and post-compression parameters were evaluated along with in vitro drug release studies, characterization studies like Fourier Transform Infra-Red spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), X-Ray Diffraction (XRD) and stability studies.
 Results: Phytochemical tests revealed the presence of starch in all extracts. Starch prepared from 0.5% sodium hydroxide (ESS4) showed best physicochemical properties. In vitro dissolution studies revealed that solid dispersion F4 containing Febuxostat and poloxamer-188 in 1:3 ratios showed better drug release. Formulation FE5 containing F4 solid dispersion with 12.5% w/w of ESS4 showed enhanced drug release. FT2 tablets having 12.5% w/w of ESS4 showed better drug release when compared to others. FTIR and DSC studies revealed no major interactions between drug and excipients. XRD studies revealed the nature of formulations. Accelerated stability studies showed that all tablets were stable.
 Conclusion: The super disintegrant property of Entada scandens seed starch was evaluated.
Highlights
Solubility is an important physicochemical factor which affects drug absorption and therapeutic effectiveness
Phytochemical screening of Entada scandens seed flour and starch extracts The raw Entada scandens seed powder and starches extracted were screened for the presence of various phytochemical constituents
The current study shows that the proportion of starch as super disintegrant has greatly influenced the dissolution parameters of various formulations
Summary
Solubility is an important physicochemical factor which affects drug absorption and therapeutic effectiveness. Scientists are focusing on the development of oral dosage forms of poor aqueous solubility drugs through various solubility enhancing approaches [1] Among these approaches, preparation of solid dispersions is one of the widely used techniques. Provides faster tablet disintegration even at low concentrations They are mixed up with a tablet and some encapsulated formulations which enhance the breakup of tablet and capsules “slugs” into smaller fragments in an aqueous environment which increases the available surface area. They promote moisture penetration and dispersion of the tablet matrix [6, 7]
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