Comparison of Different Methods for Enhancing the Dissolution Rate of Poorly Soluble Drugs: Case of Griseofulvin

The efficiency of different methods for the dissolution enhancement of the poorly soluble drug griseofulvin was evaluated. The following methods were used: micronization by milling and by precipitation from supercritical fluids and adsorption on a carrier (silica aerogel). The dissolution rate of griseofulvin from the corresponding formulations was measured in vitro. It is shown that micronization of griseofulvin particles even up to nano-scaled crystals (200 nm) results in a reasonable, but not drastic increase in the dissolution rate. At the same time, if griseofulvin is adsorbed on an amorphous carrier (hydrophilic silica aerogel), its dissolution is by far higher than that of micronized griseofulvin.

[1]  F. Rubessa,et al.  Dissolution Rate of Griseofulvin from Solid Dispersions with Poly(Vinylmethylether/Maleic Anhydride) , 1988 .

[2]  K. J. Child,et al.  Effect of Particle Size on Blood Griseofulvin-Levels in Man , 1962, Nature.

[3]  W. L. Chiou,et al.  Pharmaceutical applications of solid dispersion systems: dissolution of griseofulvin-succinic acid eutectic mixture. , 1976, Journal of pharmaceutical sciences.

[4]  N. Indurwade,et al.  Development and evaluation of occlusion complexes of Griseofulvin with cyclodextrins and their hydroxypropyl derivatives , 2002 .

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

[6]  K. Schaber,et al.  Micronization of Pharmaceutical Substances by Rapid Expansion of Supercritical Solutions (RESS): Experiments and Modeling , 2002 .

[7]  N. Rasenack,et al.  Dissolution Rate Enhancement by in Situ Micronization of Poorly Water-Soluble Drugs , 2002, Pharmaceutical Research.

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

[9]  E. Reverchon,et al.  Solubility and Micronization of Griseofulvin in Supercritical Chf3 , 1995 .

[10]  C. Chiang,et al.  Improving Dissolution Rates of Griseofulivin by Deposition on Disintegrants , 1990 .

[11]  K. S. Kumaran,et al.  Enhancement of bioavailability of griseofulvin by its complexation with beta-cyclodextrin. , 1998, Drug development and industrial pharmacy.

[12]  Michael Türk,et al.  Micronization of pharmaceutical substances by the Rapid Expansion of Supercritical Solutions (RESS): a promising method to improve bioavailability of poorly soluble pharmaceutical agents , 2002 .