中文摘要：

目的建立人血浆中磺胺甲噁唑及其代谢产物的RP—HPLC测定法，研究磺胺甲噁唑及其代谢产物N4-乙酰磺胺甲噁唑的药代动力学特征。方法血样经高氯酸预处理后，进行HPLC分析，色谱柱为Lichrospher C18（5μm，250inm×4．6mm），流动相为乙腈-水-冰乙酸-三乙胺（38：62：0．4：0．3，v／v），流速为1．0ml／min，检测波长为240／lm。结果磺胺甲噁唑和N4-乙酰磺胺甲噁唑分别在1～160μg／ml和0．5～20μg／ml的范围内浓度与峰面积线性关系良好，定量限分别为1μg/ml和0．5μg/ml，日内精密度分别为0．91％～6．83％和1．80％-7．66％，日间精密度分别为2．12％～6．09％和4．16％～8．15％，回收率分别为95．9％～106．0％和98．8％～110．3％。结论建立的人血浆中磺胺甲噁唑及其代谢产物的RP—HPLC分析方法灵敏、准确、简便，适合于磺胺甲噁唑及其代谢产物N4-乙酰磺胺甲噁唑的药代动力学研究。

英文摘要：

Objective A highly sensitive method for quantitation of sulfamethoxazole and it＇ s metabolite N4 - acetylsulfamethoxazole in human plasma was established by using a high performance liquid chromatography. Methods After taken from 20 healthy persons the plasma were treated by perchloric acid and separated by HPLC on a C18 reversed - phase column using mobile phase of acetonitrile - water - acetic acid - triethylamine （38：62：0.4：0.3, v/v/v/v）. The column temperature was maintained at 25 ℃. A constant flow - rate of 1.0 mL/min was employed throughout the analyses, and the detection was performed at UV 240 nm. Results Calibration curves, which were linear over the range of 1 to 160μg/ml for sulfamethoxazole and 0.5 to 20μg/mL for it＇ s metabolite N4 - acetylsulfamethoxazole, were analyzed contemporaneously with each batch of samples. The lower limit of quantification was 1μg/mL for sulfamethoxazole and 0.5 μg/mL for N4 - acetyl - sulfamethoxazole. The batch to batch coefficient of variation of spiked quality control samples was 8.4%, 2.9% and 2.1% at sulfamethoxazole concentrations of 1, 40 and 160 μg/mL and 9.6% , 4.4% and 4.2% at N4 - acetyl - sulfamethoxazole concentrations of 0.5, 5 and 20 μg/mL, respectively. The accuracy was calculated as the differences between given and measured mean concentration, expressed with a percentage, and was 6.0% , -4.1% and 5.7% （sulfamethoxazole） respectively and 10.3%, 0.9% and 1.2% （ N4 - acetyl - sulfamethoxazole） respectively at the above - mentioned target concentrations. Conehlsion It is considered that the method was a sensitive, accurate and simple for the determination of sulfamethoxazole and it＇ s metabolite N4 - acetyl - sulfamethoxazole in human plasma, and it has been used suc- cessfully to study pharmacokinetics of sulfamethoxazole and it＇ s metabolite in adult healthy persons.