Enhancement of griseofulvin release from liquisolid compacts.

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.

[1]  M. Barzegar-Jalali,et al.  Kinetic Analysis of Chlorpropamide Dissolution from Solid Dispersions , 2007, Drug development and industrial pharmacy.

[2]  B. El-Houssieny,et al.  Bioavailability and biological activity of liquisolid compact formula of repaglinide and its effect on glucose tolerance in rabbits. , 2010, Bioscience trends.

[3]  J. Schierholz,et al.  Have inadequate delivery systems hampered the clinical success of inhaled disodium cromoglycate? Time for reconsideration , 2011, Expert opinion on drug delivery.

[4]  Yousef Javadzadeh,et al.  The effect of type and concentration of vehicles on the dissolution rate of a poorly soluble drug (indomethacin) from liquisolid compacts. , 2005, Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques.

[5]  C. Leopold,et al.  Drug release from liquisolid systems: speed it up, slow it down , 2011, Expert opinion on drug delivery.

[6]  R. Grover,et al.  In vitro release evaluation of hydrocortisone liquisolid tablets. , 1998, Journal of pharmaceutical sciences.

[7]  Spiro Spireas,et al.  Enhancement of prednisolone dissolution properties using liquisolid compacts , 1998 .

[8]  Wolfgang Arlt,et al.  Feasibility study of hydrophilic and hydrophobic silica aerogels as drug delivery systems , 2004 .

[9]  C. Pouton,et al.  Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems. , 2000, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[10]  A. Godec,et al.  Novel hybrid silica xerogels for stabilization and controlled release of drug. , 2007, International journal of pharmaceutics.

[11]  R. Löbenberg,et al.  Modern bioavailability, bioequivalence and biopharmaceutics classification system. New scientific approaches to international regulatory standards. , 2000, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[12]  A. Nokhodchi,et al.  Effect of Some Commercial Grades of Microcrystalline Cellulose on Flowability, Compressibility, and Dissolution Profile of Piroxicam Liquisolid Compacts , 2009 .

[13]  M. Kassem,et al.  Enhancement of famotidine dissolution rate through liquisolid tablets formulation: in vitro and in vivo evaluation. , 2008, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[14]  A H de Boer,et al.  Effect of microcrystalline cellulose on liquid penetration in and disintegration of directly compressed tablets. , 1979, Journal of pharmaceutical sciences.

[15]  A. Yadav,et al.  Improvement of Solubility and Dissolution of Indomethacin by Liquisolid and Compaction Granulation Technique , 2009 .

[16]  I. Smirnova,et al.  Effect of surface functionalization of silica aerogel on their adsorptive and release properties , 2010 .

[17]  A. Nokhodchi,et al.  Enhancement of dissolution rate of piroxicam using liquisolid compacts. , 2005, Farmaco.

[18]  J. Remon,et al.  Effect of maltodextrin and superdisintegrant in directly compressible powder mixtures prepared via co-spray drying. , 2008, European journal of pharmaceutics and biopharmaceutics.

[19]  T. Osawa,et al.  Enhancement of oral bioavailability and pharmacological effect of 1-(3,4-dimethoxyphenyl)-2,3-bis(methoxycarbonyl)-4-hydroxy-6,7,8- trimethoxynaphthalene (TA-7552), a new hypocholesterolemic agent, by micronization in co-ground mixture with D-mannitol. , 1996, Biological & pharmaceutical bulletin.

[20]  I. Smirnova,et al.  In situ production of spherical aerogel microparticles , 2011 .

[21]  J. Fell,et al.  The tensile strength of lactose tablets , 1968, The Journal of pharmacy and pharmacology.

[22]  C. Leopold,et al.  Suitability of various excipients as carrier and coating materials for liquisolid compacts , 2011, Drug development and industrial pharmacy.

[23]  C. Lipinski.  Drug-like properties and the causes of poor solubility and poor permeability. , 2000, Journal of pharmacological and toxicological methods.

[24]  Yousef Javadzadeh,et al.  Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug (carbamazepine). , 2007, International journal of pharmaceutics.

[25]  Y. Asiri,et al.  In vivo evaluation of hydrochlorothiazide liquisolid tablets in beagle dogs. , 2001, International journal of pharmaceutics.

[26]  I. Smirnova,et al.  Adsorption of Drugs on Silica Aerogels , 2003 .

[27]  M. Fujii,et al.  Preparation, characterization, and tableting of a solid dispersion of indomethacin with crospovidone. , 2005, International journal of pharmaceutics.

[28]  C. Jarowski,et al.  Use of Powdered Solutions to Improve The Dissolution Rate of Polythiazide Tablets , 1990 .

[29]  R. Grover,et al.  Effect of powder substrate on the dissolution properties of methyclothiazide liquisolid compacts. , 1999, Drug development and industrial pharmacy.

[30]  I. Smirnova,et al.  Dissolution Rate Enhancement by Adsorption of Poorly Soluble Drugs on Hydrophilic Silica Aerogels , 2005, Pharmaceutical development and technology.

[31]  N. Tiong,et al.  Effects of liquisolid formulations on dissolution of naproxen. , 2009, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[32]  Ali Nokhodchi,et al.  Cogrinding as an approach to enhance dissolution rate of a poorly water-soluble drug (gliclazide) , 2010 .

[33]  Boyang Yu,et al.  Improving the solubility of ampelopsin by solid dispersions and inclusion complexes. , 2005, Journal of pharmaceutical and biomedical analysis.

[34]  An Investigation of Physicochemical Properties of Piroxicam Liquisolid Compacts , 2007, Pharmaceutical development and technology.

[35]  O. Corrigan.  Mechanisms of Dissolution of Fast Release Solid Dispersions , 1985 .

[36]  Irina Smirnova,et al.  Comparison of Different Methods for Enhancing the Dissolution Rate of Poorly Soluble Drugs: Case of Griseofulvin , 2005 .