摘要 : Pharmacokinetics (PK), pharmacodynamics (PD), and PK/PD ratios of a new solvate of enrofloxacin (enrofloxacin hydrochloride-dihydrate; enro-C), were studied in hamsters. Enrofloxacin from Baytril (R) 5% (enro(R)) served as the ref... 展开 Pharmacokinetics (PK), pharmacodynamics (PD), and PK/PD ratios of a new solvate of enrofloxacin (enrofloxacin hydrochloride-dihydrate; enro-C), were studied in hamsters. Enrofloxacin from Baytril (R) 5% (enro(R)) served as the reference preparation. Two groups of 60 Syrian golden hamsters were intramuscularly injected individually with 10 mg/kg of enro(R) or with enro-C. Tissue and serum samples were obtained for 72 h; enrofloxacin concentrations were determined by HPLC with UV detection. Ninety percent minimum inhibitory concentrations (MIC90) were determined for strains of methicillin-resistant Staphylococcus aureus, Leptospira interrogans, and Escherichia coli. All PK variables were statistically different between groups (P < 0.01). C-MAX of enrofloxacin for enro-C was 17.3 mu g/mL and it was 2.6 mu g/mL for enro R. AUC was considerably higher for enro-C (459.2 mu g/mL h vs. 19.9 mu g/mL h). There were no statistically significant differences in MIC90 values between enro(R) and enro-C. Tissue concentrations of enro-C in all cases were higher and remained above the MIC for longer periods than those of enro(R). Relevant PK/PD ratios for enrofloxacin (AUC/MIC >= 125 and C-MAX > MIC = 10-12) are consequently superior for enro-C. Given the outstanding PK/PD ratios of enro-C, this new moiety is proposed as a possible solution when high tissue concentrations of enrofloxacin are necessary. 收起