磺胺药和三甲氧苄胺嘧啶在马体内代谢动力学研究  

PHARMACOKINETICS OF SULFONAMIDES AND TRIMETHOPRIM IN HORSES

作　　者：李涛[1] 解启英 王振隆 佟恒敏[1] 乔桂林[1] 

机构地区：[1]东北农学院

出　　处：《畜牧兽医学报》1989年第3期260-265,共6页ACTA VETERINARIA ET ZOOTECHNICA SINICA

摘　　要：本文以重氮偶合比色法(以下称B-M比色法)或高效液相色谱(以下简称HPLC)法,对磺胺药和三甲氧苄胺嘧啶(TMP)在马体内代谢动力学特征进行了分析。其中磺胺二甲基嘧啶(SM_2)和TMP在血浆中的浓度用HPLC法进行测定。SM_2测定的紫外检测器波长为275nm;流动相为甲醇:去离子水(50:50/V:V)并以36％乙酸将pH调至4.0,流速为0.5ml/min;SM_2的滞留时间为8.05分钟,内标物SMM的滞留时间为9.90分钟。TMP的测定使用紫外检测器,检测波长为254nm;流动相为甲醇:双重蒸馏水:磷酸盐缓冲液(pH7.0):36％乙酸(70:30:1:1),流速为0.8ml/min。SD、SMD、SMM和SDM′的血中浓度用B-M比色法测定。血药浓度—时间数据按多室动力学处理,用Sharp PC-1500袖珍计算机计算数据,所得磺胺药和TMP的动力学参数如下:SD、SM_2、SMD、SMM、SDM′及TMP的t_(1/2)β分别为5.41±1.45、12.92±4.17、5.76±1.22、4.45±1.44、14.13±2.15及4.20±1.08(hr.);表观分布容积(Vd)分别为10.34±1.13、7.95±1.77、4.91±0.46、7.79±0.66、5.69±2.19(100ml/kg)及2.24±0.60(L/kg);曲线下面积(AUC)分别为53.42±14.81、245.14±61.35、84.37±12.73、74.78±18.36、169.74±27.13(mg％·hr.)及41.67±10.40(μg·hr./ml);清除率(Cl_B)分别为1.4476=0.5230、0.Pharmacokinetic characteristics of sult'onamides and trimethoprim ( TMP ) in healthy adult horses were studied by using B-M colorimetry or high-performance liquid chromatography procedure. The determination of SM2 and TMP were performed with a reversed-phase zorbax-ODS column (4.6mm ID×250/mm), and a wavelength of UV detector of SM2 was operated at 275 nm; the ration of methanol and water was 1:1 in the mobile phase and its pH was adjusted to 4.0 by using 36% acetic acid; a flow rate of 0.5ml/min was established; the retention time was on an average 8 minutes; the retention time of the internal standard ( SMM ) were 9.9 minutes; but the wavelength of UV detector of TMP was 254 nm; the mobile phase was methanol:water:phosphate:acetic acid (70:30: 1 : 1); a flow rate was 0.8ml/min. The data of drug concentration-time were described by the multi-compartment open models and their calculation was performed by Sharp-PC-1500 pocket computer. Pharmacokinetic parameters of sulfonamides and trimethoprim were as follows: the elimination halftime ( t1/2 ) of SD, SM2, SMD, SMM, SDM' and TMP was 5.41±1.45, 12 . 92±4.17, 5.76±1.22, 4.45±1.44, 14.13±2.15 and 4.20±1.08 ( hr. ) respectively; the apparent volume of distribution ( Vd ) was 10.34 ± 1.13, 7.95±1.77, 4.91±0.46, 7.79±0.66, 5.69±2.19 (100ml/kg) and 2.24±0.60 (1/kg) respectively; the area under curve ( AUC) was 53.42±14.81, 245.14 ± 61.35, 84.37±12.73, 74.78±18.36, 169.74±27.13 ( mg/100ml/hr. ) and 41.67±10.40(ug.hr./ml) respectively; the total body clearance ( ClB ) was 1.4476±0.5232,0.4313 ±0.1300, 0.6030 ± 0.0909, 1.3980 ± 0.3420, 0.3000±0.0400 ( 100ml/kg.hr. ) and 0.3780±0.0700 ( ml/kg.hr. ) respectively. The parameters fo multiple dosing were calculated, and then a dosage regimen was recommended for horses.

关 键 词：磺胺药 TMP 马 动力学代谢 

分 类 号：S859.7[农业科学—临床兽医学]