Effects of dairy products on the oral bioavailability of moxifloxacin, a novel 8-methoxyfluoroquinolone, in healthy volunteers.
OBJECTIVE
To investigate the effect of concomitant administration of dairy products on the pharmacokinetics and tolerability of moxifloxacin.


METHODS
This was a single-centre, randomised, controlled, nonblinded, 2-way crossover study in healthy volunteers.


METHODS
12 healthy men (aged 25 to 46 years) were enrolled in the study.


METHODS
The plasma and urinary pharmacokinetics of moxifloxacin were investigated after single doses of moxifloxacin 400mg administered orally either under fasting conditions or immediately after 250g of yoghurt that was to be consumed within 15 minutes. There was a 1-week interval between the study periods.


RESULTS
Administration of moxifloxacin after yoghurt had no effect on the extent of absorption, as estimated by the area under the plasma concentration-time curve from zero to infinity [AUCinfinty; geometric means 31.8 versus 33.9 mg/L x h after test and reference, respectively; estimated true treatment ratio 94%, 90% confidence interval (CI) 90 to 98%]. The rate of absorption was slightly decreased, with a slight reduction in maximum plasma concentration (Cmax; geometric means 2.44 versus 2.87 mg/L; estimated true treatment ratio 85%, 90% CI 74 to 98%) and a prolonged time to reach Cmax (tmax; median 2.75 versus 0.88 hours). The treatments were well tolerated in these healthy individuals.


CONCLUSIONS
The effects of yoghurt on the pharmacokinetics of moxitloxacin are considered not clinically relevant. Hence, no special recommendations for administration are required when moxifloxacin is given together with dairy products.
Stass
H
H
Pharma Research Centre, Institute of Clinical Pharmacology, Bayer AG, Wuppertal, Germany. Heino.Stass.hs@bayer-ag.de
Kubitza
D
D
D000284:Administration, Oral; D000328:Adult; D000704:Analysis of Variance; D000890:Anti-Infective Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D019540:Area Under Curve; D001372:Aza Compounds; D001682:Biological Availability; D018592:Cross-Over Studies; D003611:Dairy Products; D024841:Fluoroquinolones; D006207:Half-Life; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D008657:Metabolic Clearance Rate; D000077266:Moxifloxacin; D011804:Quinolines
D000890:Anti-Infective Agents; D001372:Aza Compounds; D024841:Fluoroquinolones; D011804:Quinolines; D000077266:Moxifloxacin