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

Acta Pharm. 57 (2007) 99-109

Short communication

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

YOUSEF JAVADZADEH¹, MOHAMMAD REZA SIAHI¹,SOLMAZ ASNAASHARI¹ and ALI NOKHODCHI¹^,2^,*

a.nokhodchi@kent.ac.uk

¹Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Iran

²Medway School of Pharmacy, Central Ave., University of Kent and Greenwich, Chatham, Kent, ME4 4TB, United Kingdom

Accepted January 9, 2007

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, 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 ^oC/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.

Keywords: indomethacin, liquisolid compacts, dissolution rate, aging, DSC, XPD