HPLC荧光法测定人血浆中的5-氨基水杨酸

Determination of 5-aminosalicylic acid in human plasma by HPLC-FLU

目的采用HPLC荧光法测定人血浆中的5-氨基水杨酸,研究单剂量口服柳氮磺吡啶肠溶片后5-氨基水杨酸在中国健康受试者体内的药动学特征。方法 24名健康受试者口服500 mg柳氮磺吡啶肠溶片,采用HPLC荧光法测定血浆中5-氨基水杨酸的浓度,利用DAS 2.1.1软件计算药动学参数。结果 5.055～808.8 ng.mL-15-氨基水杨酸与峰面积比值的线性关系良好(r=0.9985),最低检测浓度为5.055 ng.mL-1,日内、日间RSD均<10%。单次口服给药后,药动学参数为:t1/2=11.19±2.48 h,Cmax=232.83±57.94 ng.mL-1,Tmax=17.58±5.33 h,AUC(0～t)=5.5907±1.7848μg.h.mL-1。结论所用方法准确、灵敏度高、重复性好,可用于口服柳氮磺吡啶肠溶片后5-氨基水杨酸血药浓度测定及人体药动学研究。

OBJECTIVE To establish an HPLC-fluoresence method for the determination of 5-aminosalicylic acid in human plas-ma and study the pharmacokinetics in Chinese healthy volunteers following oral administration of sulfasalazine enteric-oated tablets. METHODS In the study,24 volunteers were administered with single oral dose of 500 mg of sulfasalazine enteric-coated tablets. The plasma concentrations of 5-aminosalicylic acid was determined by HPLC-fluoresence method.The pharmacokinetic parameters were calculated with aid of the software DAS 2.1.1.RESULTS The calibration curve of 5-aminosalicylic acid was linear in the range from 5.055 to 808.8 ng·mL-1 （r=0.9985）.The lowest limit of quantification of 5-aminosalicylic acid was 5.055 ng·mL-1. Both the intra-day and inter-day RSD were less than 10%.The main pharmacokinetic parameters of 5-aminosalicylic acid were as follows：t 1/2 was 11.19±2.48 h,C max was 232.83±57.94 ng·mL-1 ,T max was 17.58±5.33 h and AUC（0～t）was 5.5907±1.7848μg· h·mL-1 .CONCLUSION The HPLC-fluoresence method is precise,sensitive and reproducible.It can be used in the determination of 5-aminosalicylic acid in human plasma and clinical pharmacokinetics studies following oral administration of sulfasalazine enteric-coated tablets.