Abstract

The purpose of the present investigation was to increase the solubility and dissolution rate of flurbiprofen (FLB) by the preparation of its solid dispersion with polyethylene glycol 4000, and 6000 as carriers using solvent evaporation method (SM) and kneading method (KM). Drug polymer interactions were investigated using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), x-ray diffraction (XRD). The prepared solid dispersions were characterized by IR spectroscopy, which suggests no interaction of drug with carriers. XRD and DSC study indicates reduction in drug crystallinity. Drug solubility was more and also the dissolution was rapid for Flurbiprofen solid dispersions compared to pure drug.

Highlights

  • Oral bioavailability of a drug depends on its solubility and/or dissolution rate, and dissolution may be the ratedetermining step for the onset of therapeutic activity

  • The prepared solid dispersions were characterized by Infrared spectra (IR) spectroscopy, which suggests no interaction of drug with carriers

  • Poorly aqueous soluble drugs are usually characterized by a low bioavailability due to less absorption, which is a major concern of pharmaceutical industries worldwide (Hasnain and Nayak, 2012)

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Summary

Introduction

Oral bioavailability of a drug depends on its solubility and/or dissolution rate, and dissolution may be the ratedetermining step for the onset of therapeutic activity. Poorly aqueous soluble drugs are usually characterized by a low bioavailability due to less absorption, which is a major concern of pharmaceutical industries worldwide (Hasnain and Nayak, 2012). Techniques that have commonly been used to improve dissolution and bioavailability of poorly water-soluble drugs, in general include micronization, the use of surfactant, and the formation of solid dispersions (Sammour et al, 2006). Solid dispersion is one of the techniques that can potentially enhance the dissolution rate of hydrophobic drugs with pharmacologically inert, polymeric materials (Shin and Kim, 2003). The term ‘solid dispersion’ has been utilized to describe a family of dosage forms whereby the drug is dispersed in a biologically inert matrix, usually with a view to enhancing oral bioavailability (Craig, 2002). The improvement of solubility and dissolution rate of drugs from solid dispersions is based on mainly three different mechanisms includes; increased wettability of drug due to direct contact with hydrophilic carrier, the reduction in particle size results increased surface area, and the conversion of crystalline state to more soluble amorphous state (De Waard et al, 2008)

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