磺胺甲噁唑及其代谢产物在健康人体内的药物动力学研究  

Pharmacokinetic study of Sulfamethoxazole and metabolite in healthy chinese volunteers

作　　者：李向阳[1,2] 冯伟力[2] 程会云[2] 朱俊博[2] 格日力[2] 

机构地区：[1]沈阳药科大学生命科学与生物制药学院,辽宁沈阳110016 [2]青海大学医学院,青海西宁810001

出　　处：《华西药学杂志》2010年第1期43-45,共3页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:30460149)

摘　　要：目的探讨磺胺甲噁唑及其代谢产物N4-乙酰磺胺甲噁唑在健康男性志愿者体内的药物动力学。方法20名受试者口服复方新诺明片后,采用RP-HPLC法测定磺胺甲噁唑及其代谢产物N4-乙酰磺胺甲噁唑的血药浓度,DAS2.0软件计算药物动力学参数。结果磺胺甲噁唑及其代谢产物N4-乙酰磺胺甲噁唑的主要药物代谢动力学参数t1/2分别为9.30±1.11、12.43±2.43h,AUC0-t为1202.5±238.3、240.9±47.1μg·h·mL-1,CL为1.01±0.22、1.99±0.43L·h-1·kg-1,Vd为13.27±1.73、34.49±4.38L·kg-1,MRT为12.06±0.94、15.40±1.81h。结论磺胺甲噁唑在体内吸收迅速、消除半衰期较长,其乙酰化代谢途径为生成限速代谢模式,20名受试者中没有发现明显的快慢代谢分型。OBJECTIVE To study the pharmacokinetics of sulfamethoxazole and metabolite N^4 - acetylsulfamethoxazole in healthy Chinese volunteers. METHODS 20 healthy Chinese volunteers were administrated orally of eotrimoxazole tablets. Then the plasma concentration of sulfamethoxazole and metabolite Na - acetylsulfamethoxazole were determined by RP - HPLC, and plasma concentration - time data were analyzed by DAS 2.0 software to get the related pharmacokinetic parameters. RESULTS The main pharmacokinetic parameters t1/2 of sulfamethoxazole and metabolite N4 - aeetylsulfamethoxazole were 9.30 ± 1.11 h and 12.43 ± 2. 43 h,respectively;AUC0-t were 1202.5 ± 238.3 μg·h·mL^-1 and 240.9 ±47.1 μg·h·mL^-1 , CL were 1.01 ±0.22 L·h^-1·kg^-1 and 1.99±0.43 L·h^-1·kg^-1,Vd were 13.27±1.73 L·kg^-1 and 34.49 ± 4.38 L·kg^-1,MRT were 12.06±0.94 hand 15.40±1.81 h. CONCLUSION Sulfamethoxazole has rapid absorption and long half - life time of elimination after oral administration, and the elimination of N4 - acetylsulfamethoxazole was a formation rate - limited metabolism. Slow and fast aeetylators for sulfamethoxazole were not be found in this study.

关 键 词：磺胺甲噁唑 N^4-乙酰磺胺甲嗯唑 药物动力学 高效液相色谱 

分 类 号：R917[医药卫生—药物分析学]