Pharmacokinetics of a Long-Acting Formulation of
Azithromycin in Pigs
Lilia Gutierrez, Luis Ocampo, Ismael
Martínez, Jorge Miranda-Calderon and Hector Sumano*
Departamento de
Fisiología y Farmacología, Facultad de Medicina Veterinaria y
Zootecnia. Universidad Nacional Autónoma de México. Av. Universidad
3000, Delegación Coyoacán, Ciudad de México C.P. 04510 *Corresponding author:sumano@unam.mx
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. Cmax was 1.4 and 2.5 μg/mL, and Tmax
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 T½β 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, Cmax 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 µg/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.
Key words:
Azithromycin,
Long acting,
Peri-caudal,
Pharmacokinetics, Pig