Active Ingredients: Azithromycin
A, Villiers-le-Bel, France was used to simulate the 1 h infusion of azithromycin iv until the corresponding serum or ELF Cmax was achieved in the central compartment Cc. Flow rates in the peristaltic pumps were synchronized all over the simulated period using the Win Lin software Cole-Parmer Instrument Co.
After 4 h, to mimic the concentrations achieved in human ELF from 4 to 24 h 7 an additional reservoir, subcompartment 0 S 0, was used.
The volume of S 0 was calculated according to the volume of Cc 600 mL and the flow rate for azithromycin. Pharmacokinetic simulations Steady-state pharmacokinetic profiles in serum and ELF after an azithromycin 500 mg iv regimen were simulated over 24 h.
The clearance used in the ELF profile was calculated using a half-life of 68 h Ke; 0. Pharmacokinetic analysis Pharmacokinetic analysis was performed in triplicate, in bacteria-free simulations under the same experimental conditions.
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AZM is composed by fifteen-membered ring structure having two sugar moieties, several hydroxyl groups, two tertiary amino groups, and one oxycarbonyl group Figure 1.
It is only slightly soluble in water but highly soluble in lower alcohols and yet shows low viscosity in these solvents. These chemical modifications derived from the primary molecule erythromycin have produced profound modifications on the AZM in vitro spectrum, potency, and superior stability to acid environment.
Among other reasons, this antibiotic formulated mainly as suspension or tablets is used in human and in veterinary medicine.