Abstract

Design and characterization of intra-oral fast dissolving tablets containing diacerein-solid dispersion

Highlights

  • Diacerein (Diacetylrhein, DCN) is anthraquinone derivative of 9, 10- dihydro-4, 5 bis-9, 10-dioxo-2anthracene carboxylic acid (Fig. 1)

  • Solid dispersions (SDs) formation increased the dissolution rate of DCN compared to physical mixtures (PMs); this demonstrates that the improvement of dissolution rate with SD can be due to physical change in drug crystal which was confirmed by thermal analysis

  • The same result obtained with indomethacin (El-Badry et al, 2009) demonstrated that the ratio of indomethacin dissolved from PEG 400 solid dispersion was increased as the medicate to polymer ratio increased

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Summary

Introduction

Diacerein (Diacetylrhein, DCN) is anthraquinone derivative of 9, 10- dihydro-4, 5 bis (acetyl)-9, 10-dioxo-2anthracene carboxylic acid (Fig. 1). It possesses anti-inflammatory, anticatabolic, and pro-anabolic properties on cartilage and synovial membranes (Pavelka et al, 2016) and potentiates the production of proteoglycan and hyaluronic acid (Solignac, 2004), which are the structural components of cartilage. The solubility of ineffectively water-soluble drugs has been improved by numerous approaches, the solid dispersion technique the most widely used one (Dalvi et al, 2015). The oral absorption of poorly water-soluble drugs was enhanced by solid dispersion technique due to the increases in the dissolution rate by using water-soluble inert carriers

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