恩诺沙星及其活性代谢物在鸡体内的药物动力学

Pharmacokinetics of Enrofloxacin and Its Metabolite in Broilers

为全面了解恩诺沙星在鸡体内的动力学过程与药效的关系进行了本研究。用反向高效液相色谱法测定鸡血浆中的药物质量浓度，所得恩诺沙星ｃｉ－ｔｉ数据用ＭＣＰＫＰ计算机程序处理，代谢物环丙沙星的ｃｉ－ｔｉ数据用代谢物动力学方法处理。静注恩诺沙星后的ｃｉ－ｔｉ数据符合二室开放模型，主要动力学参数：ｔ１／２α（０．２５±０．０４）ｈ，ｔ１／２β（５．２６±０．８１）ｈ，Ｖｄ（４．５３±１．０７）Ｌ／ｋｇ，ＣＬＢ（０．６１±０．１１）Ｌ／（ｋｇ·ｈ），ＡＵＣ（１７．３９±３．９２）ｍｇ／（Ｌ·ｈ）。内服恩诺沙星的ｃｉ－ｔｉ数据，符合有吸收因素二室模型，主要动力学参数ｔ１／２ｋａ（０．４４±０．１１）ｈ，ｔ１／２α（１．１５±０．３８）ｈ，ｔ１／２β（９．１４±１．４５）ｈ，ＡＵＣ（１２．４８±２．３６）ｍｇ／（Ｌ·ｈ），ｔｍａｘ（１．７７±０．２１）ｈ，Ｃｍａｘ（１．４４±０．３１）ｍｇ／Ｌ，Ｆ７２．１８％。试验结果表明，鸡静注与内服恩诺沙星后，代谢物环丙沙星的生成及消除缓慢、分布广泛，是影响恩诺沙星疗效的重要因素。

The pharmacokinetic characteristics of enrofloxacin and its metabolite ciprofloxacin were studied in healthy broilers. Plasma concentrations of enrofloxacin and its metabolite were determined by a reversed phase high performance liquid chromatography(HPLC). The c i t i data of enrofloxacin in plasma were analysed with MCPKP program and the c i t i data of metabolite ciprofloxacin in plasma were calculated with metabolite kinetics method. The results showed that the c i t i data of enrofloxacin in plasma after intravenous administration in healthy broilers are fitted to a two compartment open model. The main pharmacokinetic parameters are as follows: t 1/2α (0.25±0.04) h, t 1/2β ( 5.26 ±0.81) h, Vd(4.53±1.07) L/kg, CL B(0.61±0.11) L/(kg·h), AUC(17.39±3.92) mg/ (L·h). The c i t i data of enrofloxacin in plasma following oral administration in healthy broilers are described by a two compartment open model with first order absorption. The main parameters are as follows: t 1/2kα (0.44±0.11) h, t 1/2α (1.15±0.38) h,t 1/2β (9.14±1.45) h, AUC(12.48±2.36) mg/ (L·h), t max (1.77±0.21) h, C max (1.44±0.31)mg/L, F 72.18%. Whether enrofloxacin was given p.o.or i.v.in the healthy broilers, the formation as well as elimination of metabolite, ciprofloxacin appears slow and its distribution wide in the body, indicating that the ciprofloxacin may be an important factor affecting the antimicrobial activity and clinical efficacy of enrofloxacin.