磺胺甲噁唑及其乙酰化代谢物的药代动力学研究  

Pharmacokinetic Study of Sulfamethoxazole and N^4-Acetyl-Sulfamethoxazol

作　　者：赵丽艳[1] 史向国[1] 张逸凡[1] 邢杰[1] 钟大放[1] 

机构地区：[1]沈阳药科大学药物代谢与药物动力学实验室,沈阳110016

出　　处：《中国临床药理学杂志》2001年第5期348-351,共4页The Chinese Journal of Clinical Pharmacology

基　　金：国家自然科学基金资助项目(NO.39930180)

摘　　要：目的；测定２０名中国男性健康受试者口服复方新诺明片（含磺胺甲噁唑８００ｍｇ）后磺胺甲噁唑（ＳＭＺ）和Ｎ４－乙酰基－磺胺甲噁唑（Ｎ４－Ａｃ－ＳＭＺ）的血药物浓度，进行药代动力学研究。方法：用反相高效液相色谱法同时测定磺胺甲噁唑和Ｎ４－乙酰基－磺胺甲噁唑的血浆浓度，并计算药代动力学参数。结果：磺胺甲噁唑和Ｎ４－乙酰基－磺胺甲噁唑的ｔｍаｘ分别为１．８３±０．７１ｈ和８．１０ ± ２．９４ｈ，Ｃｍаｘ分别为 ３７．５７±１３．５２ｍｇ·Ｌ－１和５．８９±２．９０ｍｇ·Ｌ－１，ｔ１／２分别为１０．２５±１．１６ ｈ和 １２．６５±１．４４ ｈ，ＡＵＣ０－３４分别为４８６．０±１８３．６ ｍｇ·ｈ·Ｌ－１和１３１．７±６４．１ｍｇ·ｈ·Ｌ－１，ＡＵＣ０－８分别为５６２．６±１９６．７ｍｇ·ｈ·Ｌ－１和１６２．２±８２．９ｍｇ·ｈ·Ｌ－１，ＭＲＴ分别为１５．８±１．５ｈ和２１．９±１．９ｈ。结论：磺胺甲■唑的乙酰化代谢途径为生成限速代谢模式，２０人中没有发现明显的快慢代谢分型。OBJECTIVE: The pharmacokinetics of sulfamethoxazol (SMZ) and N4-acetyl- sulfamethoxazol (N4-Ac-SMZ) were studied in 20 healthy Chinese volunteers,after an oral dose of a cotrimoxazole preparation (containing 800mg sulfamethoxazol). METHODES: The concentrations of SMZ and N4-Ac-SMZ in plasma were determined by high-performance liquid chromatography and their pharmacokinetic parameters were calculated. RESULTS: The tmax of SMZ and N4-Ac-SMZ were 1.83±0.71 h and 8. 10±2.94 h, Cmax were 37.57±13.52mg·L-1 and 5.89±2.90 mg·L-1, t1/2 were 10.25±1. 16 h and 12.65±1.44 h, AUC0-34h were 486.0±183.6 mg·h·L-1 and 131 .7 ±64.1 mg·h·L-1, AUC0-8 were 562.6±196.7 mg·h·L-1 and 162.2±82.9 mg·h·L-1, MRT were 15.8±1.5 h and 21.9±1.9 h, respectively. CONCLUTION: The elimination of N4-Ac-SMZ was a formation rate-limited metabolism. Slow and fast acetylators for sulfamethoxazole could not be distinguished in this study.

关 键 词：磺胺甲恶唑 N^4-乙酰基-磺胺甲恶唑 药代动力学 血药浓度 

分 类 号：R978.2[医药卫生—药品] R969.1[医药卫生—药学]