Lack of effect of food on the bioavailability of a new ketolide antibacterial, telithromycin.
Telithromycin is an innovative antibacterial designed for the treatment of community-acquired respiratory tract infections. This study assessed the effect of food on the bioavailability of a single oral dose of telithromycin 800 mg in healthy male subjects. Male volunteers aged 18-45 y were recruited for an open-label, single-dose, 2-period, cross-over study. In each trial period, subjects received a single oral dose of telithromycin 800 mg after an overnight fast, or after a standard high-fat breakfast. A washout period of 6-8 d separated the 2 study periods. All 18 subjects recruited (mean age 30.7 y) completed the study. Telithromycin was rapidly absorbed, reaching maximum plasma concentrations within a median of 2.50 and 2.25 h in the fasting and non-fasting states, respectively. There was no statistical difference between the non-fasting and fasting states for any of the pharmacokinetic parameters measured. The mean plasma telithromycin concentration versus time profiles for the non-fasting and fasting phases were almost superimposable. For the maximum plasma concentration and area under the curve from time 0 to infinity, the 90% confidence intervals for the mean non-fasting:fasting ratios were 83-116 and 101-123 mg x h/l, respectively; these are within 80-125% of the bioequivalence range. Telithromycin was well tolerated. The bioavailability, rate and extent of absorption of the new ketolide antibacterial telithromycin were unaffected by food.
Bhargava
Vijay
V
Aventis Pharma, Bridgewater, New Jersey 08807-0800, USA. vijay.bhargava@aventis.com
Lenfant
Bernard
B
Perret
Catherine
C
Pascual
Marie-Helene
MH
Sultan
Eric
E
Montay
Guy
G
D000293:Adolescent; D000328:Adult; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D018592:Cross-Over Studies; D004041:Dietary Fats / Q000494:pharmacology*; D018565:Food-Drug Interactions; D006801:Humans; D048628:Ketolides; D018942:Macrolides; D008297:Male; D008875:Middle Aged
D000900:Anti-Bacterial Agents; D004041:Dietary Fats; D048628:Ketolides; D018942:Macrolides; C106791:telithromycin