磺胺二甲基嘧啶在马体内的代谢动力学

本文选用高效液相色谱(HPLC),测定磺胺二甲基嘧啶(SM_2)在6匹健康成年马体内动力学。色谱柱采用反相 ODS 柱(46mm ID×250mm)。紫外检测器波长为275nm,流动相由50%甲醇与50%无离子水组成,并用36%乙酸校正 pH 至4.0,流速为0.5ml/min。SM_2的平均保留时间约为8分钟,内标物的保留时间平均9.9分钟。血药浓度—时间数据,符合多室模型,用夏普 PC—1500袖珍计算机处理数据。主要动力学参数如下:分布相半衰期(t_((1/2)α))为1.41±1.01(hr),消除相半衰期(t_(1/2)β))为12.92±4.17(hr),曲线下面积(AUC)为245.14±61.35,总表观分布容积(V_a)为7.59±1.77(100ml/kg),中央室表观分布容积(V_c)为3.49±0.61(100ml/kg),总清除率(Cl_B)为0.4314±0.13(100ml/kg·hr)。计算出多剂量给药参数如下:给药后24小时稳态下最高(C∞)max。平均(?)与最低(C∞)min 浓度分别为26,10.45与4.49(mg%);累积系数(R)为1.33,先导剂量为133(mg/kg)。本文提出,多剂量给药间隔时间为24小时。

PHARMACOKINETIC STUDIES OF SULFAMETHAZINE IN HORSES

A high-performance liquid chromatographic procedure was used to deter-mine sulfamethazine kinetics in six healthy adult horses.The HPLC was per-formed with a reversed.phase zorbax ODS column(4.6mm ID×250mm)and awavelength of UV detector were operated at 275nm.The mobile phase consistedof 50% methanol,50% water and adjusted pH to 4.0 with 36% acetic acid,aflow rate of 0.5ml/min was established,the retention time of sulfamethazinemaintained at average 8 minutes,the retention time of an internal standardwere 9 minutes.The date of drug concentration-time was described by themulti-compartment kinetics and their calculation was performed by Sharp PC-1500 pocket computer.Pharmacokinetie parameters of sulfamethazine were described as follows:the distribution half-life(t1/2α)of the drug was 1.41±1.01(hr),the eli-mination half-life(t1/2β)of the drug was 12.92±4.17(hr),the area undercurve(AUC)was 245.141±61.35(mg/100ml/hr),the apparent volume ofdistribution(Vd)was 7.59±1.77(100ml/kg),the apparent volume of the cen-tral compartment(Vc)was 3.49+0.61(100ml/kg),the total body clearanee(ClB)was 0.431±0.13(100ml/kg.hr).The parameters of multiple dose administrationwere calculated as follows:the maximum(Coo)max,average((?))and minimum(Coo)rain plateau plasma concentration at posttreatment hour 24 were 26.82(mg%),10.45(mg%)and 4.49(mg%),respeetively,the accumulation factor(R)was 1.33,the priming doses(D)was 133(mg/kg).This topic reported that theintervals of administrations for multiple dose of the drug were 24 hours.