Disposition and pharmacokinetics of azithromycin in serum and a lung tissue of two modified-release formulations compared with an immediate-release product on the market

Abstract

The aim of this study was to determine the disposition and pharmacokinetics in serum and a lung tissue homogenate in guinea pig (Cavia porcellus) of two experimental formulations of azithromycin, those were included in a modified release polymer matrix (MRF) after oral administration. The results obtained are compared with a commercial form of immediate release. 3 groups of animals were randomly formed in groups of 7 for control and 14 for each group of modified-release formulations (MRFs) were treated with a single dose of 8mg/kg of active principle. In lung tissue, comparisons of concentration of azithromycin, showed statistically significant differences between commercial product, MRF1 and MRF2. All pharmacokinetic parameters for MRF1 and MRF2 were significantly different with the exception of Cmax with respect to commercial product. The treatment of the animals with MRFs may have several benefits over treatment with azithromycin alone since could increase dosing interval for the two MRFs evaluated and reduce the frequency of application, patient stress levels and toxicological risks by accumulation of the active principle.