A Bioequivalence study of two Azithromycin tablet formulations in Indonesian healthy subjects

Journal of Bioequivalence & Bioavailability 05/2012; 4(5):048-051. DOI: 10.4172/jbb.1000111


Aim: To compare the bioavailability of two Azithromycin tablet formulations 500 mg Azivol® tablets as test
formulation and 500 mg Zithromax® tablets as reference formulation.
Methods: A single-dosed, open-label randomized two-way crossover design under fasting period with two
weeks wash-out period was evaluated in 24 subjects. For the analysis of pharmacokinetic properties, the blood
samples were drawn taken up to 120 hours after dosing. Plasma concentration of Azithromycin was determined
using liquid chromatography – tandem mass spectrometry method with TurboIon Spray mode. Pharmacokinetic
parameters AUC0-t, AUC0-∞ and Cmax were tested for bioequivalence after log-transformation of data and ratios of tmax
were evaluated non-parametrically.
Results: The point estimates and 90% confidence intervals (CI) for AUC0-t, AUC0-∞, and Cmax for Azithromycin
were 94.63% (86.27-103.81%), 95.35% (87.15-104.31%), 94.16% (80.31-110.41%) respectively.
Conclusion: These results indicated that the two formulations of Azithromycin were bioequivalent and thus may
be prescribed interchangeably.

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    ABSTRACT: The pharmacokinetics (PK) of a long acting 20% solution of azithromycin (AZ-LA) in pigs after a single peri-caudal injection at 10 and 20 mg/kg body weight was determined, using an aqueous formulation of the drug administered IV as reference, HPLC was used as analytical method. C-max was 1.4 and 2.5 mu g/mL, and T-max was 3.1 and 3.4 h, respectively for 10 and 20 mg/kg. Both preparations had 99.5% purity. Values for MRT were longer in the 10 mg/kg dose group (18.2 h) as compared to the 20 mg/kg group (16.5 h). Yet T1/2 beta was comparable between both dose levels (8.5 h vs. 7.2 h, for 10 and 20 mg/kg, respectively). No linear increments linked to dose were found in variables such as relative bioavailability, C-max and apparent volume of distribution. Values for relative bioavailability (Fr) of the higher dose as compared to the lower were 86.81% and absolute bioavailability (F) was 110.5 for the lower dose and 115.9% for the higher. Best PK/PD ratios for clinical efficacy of azithromycin describe this antibacterial drug as time-dependent. Considering pig's serum concentrations of the AZ-LA preparation here studied after its peri-caudal injection and based on a theoretical minimal therapeutic concentration in plasma of 0.1 mu g/mL based on bacteriological testing, a dose-interval of up to 48 h can be achieved. The suitability of this preparation to treat pig respiratory diseases is addressed. (C) 2014 PVJ. All rights reserved
    No preview · Article · Jan 2015 · Pakistan Veterinary Journal