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Liquisolid technique as a tool for enhancement of poorly water-soluble drugs and evaluation of their physicochemical properties Cover

Liquisolid technique as a tool for enhancement of poorly water-soluble drugs and evaluation of their physicochemical properties

Open Access
|Feb 2007

Abstract

The potential of liquisolid systems to improve the dissolution properties of a water-insoluble agent (indomethacin) was investigated. In this study, different formulations of liquisolid tablets using different co-solvents (non-volatile solvents) were prepared and the effect of aging on the dissolution behaviour of indomethacin liquisolid compacts was investigated. To evaluate any interaction between indomethacin and the other components in liquisolid formulations, X-ray powder diffraction (XPD) and differential scanning calorimetry (DSC) were used. Dissolution test was carried out at two different pH, 1.2 and 7.2, to simulate the stomach or intestine fluid, respectively. The results showed that liquisolid formulations exhibited significantly higher drug dissolution rates at pH 1.2 and 7.2 compared to compacts prepared by the direct compression technique. The enhanced rate of indomethacin dissolution from liquisolid tablets was probably due to an increase in wetting properties and surface area of drug particles available for dissolution. In order to investigate the effect of aging on the hardness and dissolution rate of liquisolid compacts, the formulations were stored at 25 °C/75% relative humidity for a period of 12 months. The results showed that aging had no significant effect on dissolution profiles of liquisolid tablets. Liquisolid compacts containing propylene glycol as vehicle produced higher dissolution rates in comparison with liquisolid compacts containing PEG 400 or Tween 80 of the same concentration. The DSC and XPD results showed no changes in crystallinity of the drug and interaction between indomethacin and excipients (Avicel and silica) during the process.

DOI: https://doi.org/10.2478/v10007-007-0008-6 | Journal eISSN: 1846-9558 | Journal ISSN: 1330-0075
Language: English
Page range: 99 - 109
Published on: Feb 28, 2007
Published by: Croatian Pharmaceutical Society
In partnership with: Paradigm Publishing Services
Publication frequency: 4 issues per year
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© 2007 Yousef Javadzadeh, Mohammad Siahi, Solmaz Asnaashari, Ali Nokhodchi, published by Croatian Pharmaceutical Society
This work is licensed under the Creative Commons License.

Volume 57 (2007): Issue 1 (March 2007)