Although many basic and clinical studies have shown that glucosamine (GlcN) improves osteoarthritis, it has not been widely used in the clinic because its bioavailability is only 6%. We investigated the influence of dosing-time factors, which influence pharmacokinetics and food intake in rats to improve its bioavailability. When GlcN was orally administered to rats housed under conditions of free access to food for 12 h or fasting conditions, no significant differences in GlcN concentration were observed in the rat plasma between the two groups. There were no significant differences in the plasma GlcN concentrations among the dosing-time groups when GlcN was orally administered at 4:00, 10:00, 16:00, or 22:00 h to rats. However, the plasma concentration in the fasted group was significantly higher than that in the fed group after GlcN was orally administered at 22:00 h in rats and the AUC of the fasted group was 1.7-fold higher than that of the fed group. In conclusion, the pharmacokinetics of GlcN was improved by considering not only food intake but also the circadian rhythm of its transporter, which is a major factor influencing pharmacokinetic changes.
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