EFFECT OF FOOD ON THE BIOAVAILABILITY OF GRISEOFULVIN FROM MICROSIZE AND PEG ULTRAMICROSIZE (GRIS-PEGR) PLAIN TABLETS

抄録

Effect of food on the bioavailability of griseofulvin from its two plain tablets, a commercial microsize product and a PEG ultramicrosize (GRIS-PEG^R) one, was investigated. The drug was dissolved at a slower rate from ultramicrosize formulation than from microsize one in 18 1 of pH 7.2 buffer but at a little faster rate in 40% dimethylformamide. When administered to fasting subjects, the microsize product showed higher serum levels and peak serum level than ultramicrosize one but the extent of the bioavailability was nearly the same. A standard breakfast enhanced the rate of absorption of the drug from both the products, especially from ultramicrosize one, and those products were equivalent in the rate and extent of bioavailability after food ingestion. The peak serum level of ultramicrosize product in nonfasting was about twice higher than that in fasting subjects. The different intensities of food effect on the bioavailabilities from two dosage forms suggest that formulation factors should be considered for the evaluation of food effect.