Lack of effect of food on the bioavailability of a new ketolide antibacterial, telithromycin.

ABSTRACT

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-fastingfasting 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.