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Physicochemical characterization and pharmacokinetics in broiler chickens of a new recrystallized enrofloxacin hydrochloride dihydrate
Author(s) -
Gutierrez L.,
MirandaCalderon J. E.,
GarciaGutierrez P.,
Sumano H.
Publication year - 2015
Publication title -
journal of veterinary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.527
H-Index - 60
eISSN - 1365-2885
pISSN - 0140-7783
DOI - 10.1111/jvp.12153
Subject(s) - enrofloxacin , cmax , broiler , bioavailability , pharmacokinetics , minimum inhibitory concentration , chemistry , pharmacology , veterinary medicine , food science , medicine , antibiotics , biochemistry , ciprofloxacin
Enrofloxacin, a key antimicrobial agent in commercial avian medicine, has limited bioavailability (60%). This prompted its chemical manipulation to yield a new solvate‐recrystallized enrofloxacin hydrochloride dihydrate entity (enro C ). Its chemical structure was characterized by means of mass spectroscopy, Fourier transformed infrared spectroscopy, X‐ray powder diffraction, and thermal analysis. Comparative oral pharmacokinetics ( PK ) of reference enrofloxacin (enro R ) and enro C in broiler chickens after oral administration revealed noticeable improvements in key parameters and PK/PD ratios. Maximum serum concentration values were 2.61 ± 0.21 and 5.9 ± 0.42 μg/mL for enro R and enro C , respectively; mean residence time was increased from 5.50 ± 0.26 h to 6.20 ± 0.71 h and the relative bioavailability of enro C was 336%. Considering C max / MIC and AUC / MIC ratios and the MIC values for a wild‐type Escherichia coli O78/H12 (0.25 μg/mL), optimal ratios will only be achieved by enro C (C max / MIC = 23.6 and AUC / MIC = 197.7 for enro C ; vs. C max / MIC = 10.4 and AUC / MIC = 78.1 for enro R ). Furthermore, enro C may provide in most cases mutant prevention concentrations (C max / MIC ≥ 16). Ready solubility of powder enro C in drinking water at concentrations regularly used (0.01%) to provide an additional advantage of enro C in the field. Further development of enro C is warranted before it can be recommended for clinical use in veterinary medicine.