鸡静注和口服盐酸沙拉沙星的药物动力学研究

PHARMACOKINETICS OF SARFLOXACIN HYDROCHLORIDE IN CHICKENS AFITER INTRAVENOUS AND ORAL ADMINISTRATION

伊利莎蛋鸡８只单次快速静脉注射盐酸沙拉星１０ｍｇ／ｋｇ（以沙拉沙星计）后，利用高效液相色谱法测定血清中沙拉星的浓度。房室模型分析表明：血药浓度－时间数据适合无吸收因素二室模型，其消除半衰期（ｔβ）、表观分布容积（Ｖｄ）、总体清除率（ＣＬＢ）和药时曲线下面积（ＡＵＣ）分别为（２．４７±０．８７Ｏｈ、（５．１０±２．２５）Ｌ／ｋｇ、（１．４２±０．２４）Ｌ／ｋｇ·ｈ和（７．２７±１．３７）μｇ／ｍｌ·ｈ。伊利莎蛋鸡８只口服盐酸沙拉沙星溶液１０ｍｇ／ｋｇ（以沙拉沙星计）后，药物在体内呈现有吸收单室模型，其吸收半衰期（ｔｋａ）、消除半衰期（ｔｋｅ）、血药达峰时间（Ｔｍａｘ）、药峰浓度（Ｃｍａｘ）和药时曲线下面积分别为（０．３２±０．１５）ｈ、（３．６８±０．８９）ｈ、（１．２５±０．３５）ｈ、（０．８６±０．２８）μｇ／ｍｌ和（５．５３±１．９５）μｇ／ｍｌ·ｈ。鸡内服盐酸沙拉沙星混悬剂（以淀粉混）１０ｍｇ／ｋｇ（以沙拉沙星计）后，药物吸收不规则，统计矩理论分析表明：药时曲线零阶矩（ＡＵＣ）、药时曲线一阶矩（ＭＲＴ，平均驻留时间）和消除半衰期（ｔｋｅ）分别为（１．０３±０．２７）μｇ／ｍｌ·ｈ、（６．２２±０．７６?

A dose of 10 mg sarafloxaxin/kg body weight was administered intravenously to 8 healthy chickens. Serum sarafloxacin concentrations were determined using HPLC method. The serum concentration time date of sarafloxacin were best described by a two compartment open model. The elimination half life( t 1/2β ), the volume of distribution [ V d(area)], the total body clearance ( C l B) and the area under the curve ( AUC ) were 2.47±0.87 h, 510±2.25 L/kg, 1.42±0.24 L/kg.h and 7.27±1.37 μg/mg.h., respectively. Solution formulation of the drug was given to 8 healthy chickens at a dosage of 10 mg per kilgram of body weight orally. Serum sarafloxacin pharmacokinetic parameters were calculated using a one compartment open model. The absorption and elimination half lives were 0.32±0.15 h and 3.68±0.9 h respectively. The peak of serum concentration ( C max ) and the time to reach C max ( T max ) were 0.86±0.28 μg/ml and 1.25±0.35 h, respectively. The bioavailability( F ) was 76.03%. Following oral adminstration of the drug (suspension formulation) at a dose of 10mg sarafloxacin/kg body weight, the serum concentration time data were analysed by statistical matrix method. The area under the curve( AUC ), the mean residual time( MRT ) and the elimination half life were 1.03±0.27 μg/ml.h, 6.22±0.76 h and 2.81±0.59 h. The bioavailability( F ) was 14.22 % only.