PHARMACOKINETICS AND PHARMACODYNAMICS OF 2 ORAL FORMS OF CEFUROXIME AXETIL

Cefuroxime axetil is a cefuroxime eater that can be administered by mo uth. Two dosage forms (tablets and granules) have been developed for o ral administration. We evaluated the pharmacokinetics and pharmacodyna mics of these forms in an open cross-over study involving 12 healthy v olunteers receiving single doses of 250 mg. The bioavailability of the two forms was different, the observed peak concentration and time-con centration curve values of the tablet form being, respectively, 39 and 27% higher than those of the granule form. However, ex vivo studies o f serum bactericidal activity against Streptococcus pneumoniae showed no significant differences between the two formulations. This is in ke eping with the fact that the bactericidal activity of samples from onl y six subjects gave evaluable data for Haemophilus influenzae; althoug h small differences were found between the two formulations, further i nvestigations are required. The pharmacodynamic approach is becoming a n essential element in determining the equivalence of antibiotic dosag e forms.