Enhancement of griseofulvin release from liquisolid compacts |
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Authors: | CM HentzschelM Alnaief I SmirnovaA Sakmann CS Leopold |
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Institution: | a Institute of Pharmacy, Department of Pharmaceutical Technology, University of Hamburg, Hamburg, Germany b Institute of Thermal Separation Processes, Hamburg University of Technology, Hamburg, Germany |
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Abstract: | The potential of hydrophilic aerogel formulations and liquisolid systems to improve the release of poorly soluble drugs was investigated using griseofulvin as model drug. The in vitro release rates of this drug formulated as directly compressed tablets containing crystalline griseofulvin were compared to aerogel tablets with the drug adsorbed onto hydrophilic silica aerogel and to liquisolid compacts containing the drug dissolved or suspended in PEG 300. Furthermore, the commonly used carrier and coating materials in liquisolid systems Avicel® and Aerosil® were replaced by Neusilin®, an amorphous magnesium aluminometasilicate with an extremely high specific surface area of 339 m2/g to improve the liquisolid approach.Both the liquisolid compacts containing the drug dissolved in PEG 300 and the aerogel tablets showed a considerably faster drug release than the directly compressed tablets. With liquisolid compacts containing the drug suspended in PEG 300, the release rate increased with rising fraction of dissolved drug in the liquid portion. It could be shown that Neusilin® with its sevenfold higher liquid adsorption capacity than the commonly used Avicel® and Aerosil® allows the production of liquisolid formulations with lower tablet weights. |
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Keywords: | BCS biopharmaceutics classification system SEDDS self-emulsifying drug delivery system PEG polyethylene glycol RH relative humidity LS liquisolid RESS rapid expansion from supercritical solutions |
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