Food and muzolimine interaction.
The influence of food on the bioavailability of muzolimine was investigated in a non-controlled cross-over study. Six healthy volunteers received 40 mg muzolimine directly after a standardized American breakfast (non-fasting volunteers) and, one week later, after an overnight fast with breakfast 90 min after drug intake (fasting volunteers). The concentrations of muzolimine in plasma and urine were determined between 0 and 48 h after administration. Results (means +/- SEM): in the fasting volunteers, the areas under the muzolimine plasma level curves (0-32 h) were higher than in the non-fasting volunteers (3002 +/- 390 vs. 2038 +/- 344 ng X h/ml, p less than 0.001), the peak concentrations were higher (332 +/- 36 vs. 176 +/- 38 ng/ml, p less than 0.05) and appeared earlier (1.8 +/- 0.2 h vs. 4.0 +/- 0.5 h, p less than 0.01). Also, the urinary volumes and sodium excretion were higher in the fasting volunteers than in the non-fasting volunteers. Hence, the bioavailability of muzolimine is reduced if administered after a meal which should be considered in the treatment schedule.
D000328:Adult; D001682:Biological Availability; D005502:Food; D006801:Humans; D007700:Kinetics; D008297:Male; D009156:Muzolimine / Q000097:blood / Q000378:metabolism*; D011188:Potassium / Q000652:urine; D011720:Pyrazoles / Q000378:metabolism*; D012964:Sodium / Q000652:urine
D011720:Pyrazoles; D009156:Muzolimine; D012964:Sodium; D011188:Potassium