Absorption characteristics of solid dispersed and micronized griseofulvin in man

✍ Scribed by Win Loung Chiou; Sidney Riegelman

• Publisher: John Wiley and Sons
• Year: 1971
• Tongue: English
• Weight: 583 KB
• Volume: 60
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600600919

✦ Synopsis

Griseofulvin dispersed in polyethylene glycol 6000, prepared by the melting or solvent method, was found to be completely and rapidly absorbed after oral administration to two human subjects. The absorption from the commercially available, micronized griseofulvin was irregular and incomplete (and the average was only 4 5 z of the dose absorbed). In addition, the absorption process from the commercial product was found to continue for up to 3 days after administration.

Keyphrases 0 Griseofulvin, solid dispersion-absorption kinetics, man 0 Absorption kinetics, oral-griseofulvin solid dispersion, man Although application of solid dispersion systems to increase rates of dissolution and oral absorption of poorly water-soluble or insoluble drugs was proposed in 1961 (l), its potential and practical application in clinical therapeutics was only recently demonstrated in this laboratory in dogs (2). The drug tested was griseofulvin, which is a water-insoluble and neutral antibiotic. The dispersion of griseofulvin in a solid matrix of polyethylene glycol 6000 was found to give rise to a much higher and more constant absorption than that of the micronized products. This paper reports on the verification of these results in man. Not only does this finding have potential importance to griseofulvin therapy, it also may lead to a new mechanism for the formulation of other poorly soluble or insoluble drugs.