摘要
目的分析磺胺嘧啶在家兔体内药动学过程。方法20只家兔耳缘静脉快速推注磺胺嘧啶300mg·kg-1,752紫外分光光度计比色法测定不同时间的血药浓度并计算药动学参数。结果磺胺嘧啶在家兔体内药-时曲线符合二室模型,并表现为快慢两种速率类型。慢消除型药动学参数为:VC=(0.24±0.09)L·kg-1,V=(0.62±0.22)L·kg-1,AUC=(0.11±0.05)g.h.mL-1,CL=(3.8±1.5)mL·min-1,t1/2α=(3.3±1.3)min,t1/2β=(122±21)min。快消除型药动学参数为:VC=(0.19±0.10)L·kg-1,V=(0.45±0.17)L·kg-1,AUC=(0.062±0.022)g·h·mL-1,CL=(6.0±2.4)mL·min-1,t1/2α=(2.1±0.9)min,t1/2β=(53±5)min。与慢消除型比较,快消除型AUC减少,CL增加,P<0.05;t1/2β缩短,P<0.001。结论磺胺嘧啶在家兔体内药动学过程表现为快慢两种速率类型。快消除型AUC减少,CL增加,t1/2β缩短。本实验为磺胺嘧啶的临床给药方案制定提供了实验依据。
OBJECTIVE To analyze pharmacokinetic parameters of sulfadiazine in rabbits. METHODS A single dose of 300 mg·kg^-1 sulfadiazine was given intravenously to 20 healthy rabbits. The concentrations of sulfadiazine in different time and were determined by ultraviolet spectrophotometer and pharmacokinetic parameters were calculated. RESULTS The time-concentration curve of sulfadiazine in rabbit coincided with the two-compartment open model. Slow and fast rate-metabolism for sulfadiazine were distinguished in this study. The pharmacokinetic parameters of slow rate-metabolism were as follows ： Vc （0. 24±0. 09） L·kg^-1, V（0. 62±0. 22 ） L·kg^-1, AUC （0. 11 ± 0. 05 ） g·h·mL^-1, CL（3.8 ± 1.5 ） mL·min^-1, t 1/2α （3.3 ±1.3 ） min, t1/2β （ 122 ± 21 ） min. The pharmacokinetic parameters of fast rate-metabolism were as follows： Vc（0. 19 ±0. 10）L·kg^-1 , V（0. 45±0. 17）L·kg^-1 ,AUC（0. 062±0. 022）g·h·mL^-1, CL（6.0 ±2. 4）mL·min^-1,t1/2α （2. 1 ±0. 9） min, t 1/2β （53 ± 5 ） min. When being compared with that of slow rate-metabolism, AUC ,t1/2β of fast rate-metabolism were significantly decreased, CL of fast rate-metabolism was significantly increased. CONCLUSION Slow and fast rate-metabolism for sulfadiazine in rabbit can be distinguished. This study provides a scientific basis for clinical use of sulfadiazine.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2007年第22期1733-1735,共3页
Chinese Pharmaceutical Journal
关键词
磺胺嘧啶
家兔
药动学
sulfadiazine
rabbit
pharmacokinetics
