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;冯伟力;程会云;朱俊博;格日力;
Author:
收稿日期: 年卷(期)页码:2010,25(01):-43-45
期刊名称:华西药学杂志
Journal Name:WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字:磺胺甲噁唑;N4-乙酰磺胺甲噁唑;药物动力学;高效液相色谱
Key words:
基金项目:国家自然科学基金资助项目(批准号:30460149)
中文摘要
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。
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