Pharmacokinetics and the active metabolite of enrofloxacin in Chinese mitten-handed crab (Eriocheir sinensis)

The pharmacokinetics and active metabolite of enrofloxacin were estimated after single intramuscular administration (10.0 or 20.0 mg/kg body weight) to the Chinese mitten-handed crab (Eriocheir sinensis) in fresh water at 25.0 ± 1.0 °C. Levels of enrofloxacin and its metabolite ciprofloxacin in the main tissues (hemolymph, hepatopancreas, muscle, ovary and spermary) were simultaneously detected by HPLC. Enrofloxacin concentration–time profiles for the hemolymph in both tests were described by a two-compartment open model with first-order absorption. Distribution half-time (T1/2α), elimination half-time (T1/2β), body clearance (CL/F), mean residence time (MRT0–∞), area under the concentration–time curve from 0 to ∞ h (AUC0–∞) and apparent volume of distribution (Vd/F), which derived from the pharmacokinetic model, were 0.427 h, 21.3 h, 0.133 l/h/kg, 60.0 h, 96.9 μg/ml/h and 4.08 l/kg, respectively, at a dose of 10.0 mg/kg body weight, and 0.216 h, 12.3 h, 0.189 l/h/kg, 85.8 h, 187 μg/ml/h and 3.35 l/kg, respectively, at a dose of 20.0 mg/kg body weight. Similarities were found between the hemolymph concentration–time curves of the two tests; for example, instant absorption process followed by the distribution phrase, and a second absorption peak at 6 h post-treatment. After intramuscular administration of 10.0 mg/kg body weight, absorption of enrofloxacin was observed in the main edible tissues (hepatopancreas, muscle, ovary and spermary), and the drug residue was the highest in the hepatopancreas, where the ‘drug sink’ phenomenon occurred. Comparative pharmacokinetics showed fast absorption, broad distribution and fast elimination of enrofloxacin in E. sinensis after intramuscular dosing. Regarding ciprofloxacin, the main active metabolite of enrofloxacin, though relatively low levels were detected in all the main tissues of the crab, its kinetics in the hemolymph in the two tests were not described by a one- or two-compartment open model.