先锋霉素Ⅰ在马体内代谢动力学特征的研究  

STUDY ON THE PHARMACOKINETIC CHARACTERISTICS OF CEPHALOTHIN I IN HORSES

作　　者：佟恒敏[1] 乔桂林[1] 王振隆 李涛[1] 

机构地区：[1]东北农学院药理教研室

出　　处：《东北农学院学报》1989年第3期243-248,共6页

摘　　要：本文选用高效液相色谱(HPLC),测定先锋霉素I在4匹成年健康重挽马体内动力学过程。色谱柱采用反相ODS柱[25×4.6mm(ID))柱温35℃,流动相由甲醇:双重蒸馏水:36％醋酸:1.77％磷酸盐缓冲液(40:60:0.1:6)组成。流速为0.8 ml/min。紫外检测器波长为245nm。用高效液相色谱仪测定了不同时间血药浓度数据,符合开放式二室模型,用夏普PC—1500袖珍计算机处理数据。主要动力学参数如下:消除半衰期(t1/2β)为0.50±015(小时),分布半衰期(t1/2α)为0.05±0.01(小时),曲线下面积(AUC)为49.122±29.01(微克/毫升·小时),总表现分布容积(V_d)为0.3050±0.1488(升/公斤),总清除率(CIB)为0.3877±0.1418(毫升/公斤·小时),有效浓度维持时间[TCP(ther)]为2.78±0.49(小时)。按单剂量给药有关参数计算出多剂量给药参数如下:给药间隔时间(τ)为4小时,积累系数(R)为1.00,最高[(C∞)_(man))、平均(C)与最低((C∞)_(min)]稳态浓度分别为223.99(微克/毫升)、12.28(微克/毫升)与0.06(微克/毫升)。首次剂量(D_0~*)为15(毫克/公斤)。A high—performance Liquid chromatography (HPLC) procedure was used to determine cephalothin kinetics in four healthy adult horses. The HPLC was performed with a reversed—phase Zorbax ODS column[25mm×4.6mm^2(ID)]. The column temperatures was 35℃, The mobile phase consisted of methanol: water: 36%acetic acid: 1.77% phosphate buffer. The flow rate was 0.8ml/min. A wavelength of UV detector operated at 245nm.Cephalothin concentration in plasma at different time was determined by HPLC.The data of drug concentration-timefi tted to two-compartment open model and their calculation were performedr by sharp PC—1500 pocket computer.Their pharmacokinetic parameters of cephalothin were described as follows: Biological half-life(tl/2β)of the drug was 0.50±0.15(hr), the distribution half—life(t1/2α) of the drug was 0.05±0.01 (hr), the area under curve (AUC)was 49.122±29.01(μg/ml.hr), the apparent volume of distribution (V_d) was 0.305±0.1488 (L/kg), the total body clearance(CIB) was 0.3877±0.1418 (ml/kg·hr),tcp (ther) was 2.78±0.49 (hr).The parameters of multiple dose administration were calculated as follows:The intervals of adminisrtation for multiple dose of the drug (τ) were 4 (hr), the accumulation factor (R) was 1.00, the maximum [(C∞)max], average(C) and minimum[(C∞)min] plateau plasma concentration were 223.99(μg/ml) 12.28(μg/ml)and 0.06 (μg/ml) respectively, the loading dose (D_0~*) was 15.00 (mg/kg).

关 键 词：马体 先锋霉素Ⅰ 药物代谢动力学 

分 类 号：S858.210.4[农业科学—临床兽医学]