摘要
目的建立同时测定血浆中格列美脲及其活性代谢物羟基格列美脲(M1)的HPLC-MS/MS分析方法,研究其在健康人体的药代动力学和安全性。方法22名健康男性受试者单剂量口服格列美脲片2mg,按规定时间点取血并测定血浆中的格列美脲及代谢物M1的浓度,采用WinNonlin软件计算药代动力学参数。结果格列美脲和代谢物M1的Tmax分别为2.7±0.6和4.2±1.6h,Cmax分别为188±52和34±11μg·L-1,AUC0-24分别为813±277和258±66μg·h·L-1,t1/2分别为6.6±2.1和6.3±2.5h。结论本文所建立的HPLC-MS/MS同时测定格列美脲及其代谢物M1的方法灵敏、准确、可靠,格列美脲耐受性较好,在国人与白种人体内的药代动力学特征存在种族差异。
AIM： To establish an HPLC-MS/MS method for the simultaneous determination of glimepiride and its hydroxy-metabolite M1 in human plasma, and to study their pharmacokinetic profiles in healthy Chinese volunteers. METHODS： A single oral dose of 2 mg glimepiride tablet was given to 22 healthy male volunteers individually. The concentrations of glimepiride and M1 in plasma were determined and their pharmacokinetic parameters were simulated by WinNonlin software. RESULTS： The main pharmacokinetic parameters of glimepiride and M1 were as follows： Tmax2.7 ±0.6 and 4.2 ±1.6 h, Cmax 188±52 and 34±11 μg·L^-1, AUC0-24 813±277and 258±66 μg·h·L^-1, t1/2 6.6±2.1 and 6.3±2.5 h. CONCLUSION： The HPLC-MS/MS method developed in our lab was sensitive and precise. Glimepiride was well tolerated and exhibited ethnic difference between Chinese and Caucasian.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2006年第8期868-872,共5页
Chinese Journal of Clinical Pharmacology and Therapeutics
基金
863国家攻关项目临床试验关键技术及平台研究(№2002AA2Z341A
2004AA2Z3760)
