Bioavailability of griseofulvin from tablets in beagle dogs and correlation with dissolution rate and bioavailability...

The bioavailability of four griseofulvin tablets in beagle dogs, including an ultramicrosize tablet used previously in a human bioavailability study, was investigated on the basis of the plasma 6-demethyl-griseofulvin concentration. The relations with the in vivo findings in humans and the in vitro dissolution rates also were examined. Contrary to the lower bioavailability of the ultramicrosize formulation in humans, it provided the best bioavailability in beagles. The microsize griseofulvin formulations showed similar in vivo results to those in humans. Poor correlation of in vivo parameters between humans and beagles was attributed to the discrepancy of the availability of the ultramicrosize formulation between the two species. The dissolution rates determined by the pretreatment method using plastic beads were correlated more with the in vivo findings than those determined by the other methods. Beagles were a useful animal model for bioavailability studies of certain griseofulvin formulations but not ultramicrosize ones.