HPLC-MS/MS研究阿奇霉素片人体药动学  

Pharmacokinetics Study of Azithromycin Tablets in Health Volunteers by HPLC-MS/MS

作　　者：王华[1] 申屠建中[2] 陈雪帆[3] 黄巧巧[3] 金一[4] 

机构地区：[1]浙江大学分析测试中心,杭州310029 [2]浙江大学医学院附属第一医院临床药理研究室,杭州310003 [3]浙江省药品检验所,杭州310029 [4]浙江大学药学院,杭州310029

出　　处：《中国药学杂志》2006年第18期1414-1416,共3页Chinese Pharmaceutical Journal

摘　　要：目的 建立HPLC-MS/MS检测体内阿奇霉素血药浓度,并用于研究阿奇霉素片人体药动学.方法 应用建立的HPLC-MS/MS方法测定人血清中阿奇霉素的浓度,并通过PKs软件进行房室模型拟合,计算主要药动学参数.结果 阿奇霉素的线性范围为3.33～833μg·L-1,方法回收率为100%～115%,日内、日间RSD值均小于6%,人po阿奇霉素500 mg后的药-时曲线均符合二房室开放模型,其主要药动学参数t1/2α为（2.93±3.38）h,t1/2β为（36.24±8.34）h,t1/2ka为（0.61±0.34）h,ρmax为（415.9±114.4）μg·L-1,tmax为（1.812±0.650）h,AUC0-t为（6 937±1 626）μg·h·L-1,CL/F为（0.076±0.018 2）L·h^-1,Vd/F为（3.976±1.413）L,tlag为（0.349±0.173）h,k10为（0.110±0.039）h^-1,k21为（0.067±0.025）h^-1,k12为（0.223±0.109）h^-1.结论 该法简便、灵敏、特异,适用于阿奇霉素片人体药动学研究.OBJECTIVE To establish HPLC-MS/MS method for the determination of azithromycin in human serum, study pharmacokinetics of azithromycin in healthy volunteers. METHODS azithromycin in serum were determined by LC-MS/MS and the pharmacokinetic parameters were calculated by PKs program. RESULTS The linear regressive curves were obtained in the range of 3.33 - 833 μg· L^-1. Recoveries using the method of azithromyein was 100% - 115%. The within-day and betweenday RSDs were less than 6%. After oral admination of azithromyein tablets in 18 healthy volunteers , the pharmaeokinetive process was fitted to the two-compartment mode, the main pharmaeokineties parameters were ： t1/2α（2.93 ± 3.38）h, t1/2β（36.24 ± 8.34）h, t1/2ka（0.61 ± 0.34） h, ρmax（415.9 ± 114.4） ng·mL^-1, tmax（ 1.812 ± 0.650）h, AUC0-t（6937 ± 1626） μg· h· mL^-1, CL/F（0.076 ± 0.0182） L· h^-1, Vd/F（3.976 ± 1.413） Llog（0.349 ± 0.173） h, k10 （0.110±0.039）h^-1, k21 （0.067 ± 0.025） h^-1 and k12（0.223 ± 0.109）h^-1 .CONCLUSION HPLC-MS/MS method established in this study is simple, sensitive with good accuracy and precision, which can be adapted to pharmacokinetics study.

关 键 词：阿奇霉素 液相色谱-质谱/质谱 药动学 

分 类 号：R969.1[医药卫生—药理学]