中文摘要：

目的探讨磺胺甲噁唑及其代谢产物N^4-乙酰磺胺甲咏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N^4-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N^4-乙酰磺胺甲嗯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，AUC0-1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。

英文摘要：

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.