Absorption kinetics of griseofulvin in man

✍ Scribed by M. Rowland; S. Riegelman; W. L. Epstein

• Publisher: John Wiley and Sons
• Year: 1968
• Tongue: English
• Weight: 628 KB
• Volume: 57
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600570613

✦ Synopsis

The distribution and elimination kinetics of griseofulvin have been examined in man. T h e drug was administered intravenously in polyethylene glycol 300 via a saline drip. The plasma-concentration time cuwe was satisfactorily described by a bi-exponential equation, the half-life for the first exponent was found to be 0.70-1.7 hr. and the second 9.5-21.0 hr. It was also shown that the area under theplasmaconcentration time curve was proportional to the dose administered. Griseofulvin was then given orally and from the plasma concentration, the kinetics of the absorption of this drug were calculated. Absorption was found to occur up to 30 hr. after administration and 27-72.5 percent of the dose was absorbed. INCE ITS introduction in 1958 (1) griseofulvin S still remains the only effective oral antifungal agent for the treatment of dermatophytic infections and much interest has been shown in the absorption of this drug. It was the evidence of Sharp and Tomich (2), that the oral toxicity in rats and mice was much lower than that following intraperitoneal administration, which first led to the suggestion that griseofulvin may be incompletely absorbed. This was confirmed b y Davis et al. (3) who recovered 30-64% of an oral dose in the feces of rats. Numerous workers have since shown inefficient absorption of griseofulvin in man and have increased the degree of absorption by reduction of particle size (4-9),