阿扎他定血药浓度的测定及其药动学的研究  

Studies on Determination and Pharmacokinetics of Azatadine in Human Plasma by LC-MS-MS

作　　者：马忠英[1] 朱艳荣[1] 乔逸[1] 石小鹏[1] 冯娟[1] 周伦[1] 常瑛[1] 刘渝[1] 赵培西[1] 文爱东[1] 

机构地区：[1]第四军医大学西京医院药剂科,西安710032

出　　处：《抗感染药学》2012年第4期273-276,共4页Anti-infection Pharmacy

摘　　要：目的:应用LC-MS-MS法研究抗组胺药物马来酸阿扎他定片的人体药动学特征.方法:10名健康受试者分别口服马来酸阿扎他定片1mg和2mg,采用LC-MS-MS法测定给药后0～48h内人体血浆中阿扎他定的浓度,并计算其药动学参数.结果:阿扎他定质量浓度的线性范围为0.05～5.00ng/mL,最低定量下限为0.05ng/mL,主要药动学参数分别为tmax为(3.90±0.994)h,(3.70±1.059)h;Cmax为(0.795±0.187)ng/mL,(1.444±0.245)ng/mL;t1/2为(11.716±2.005)h,(10.62±2.06)h;AUC0～48为(11.213±4.042)ng·h/mL,(18.80±6.98)ng·h/mL。结论:本法操作简便、灵敏度高、干扰少、结果准确的优点,适用于阿扎他定药动学的研究。Objective： To study the pharmacokinetics of oral azatadine maleate at once and multiple-dose in Chinese healthy volunteers by LC-MS-MS. Methods： 10 healthy volunteers were administrated 1 mg or 2 nag azatadine maleate a day once.The plasma concentrations were determined by LC-MS-MS. The phannacokinetic parameters were calculated by DAS 2.0 software. Results： The limits of quantitation of method for azatadine was 0.05 ng/m and the linear range of the calibration curves in plasma was between 0.05 and 5.00 ng/mL. The pharmacokinetic parameters were as follows： tmax was （ 3.90±0.994）h, （ 3.70± 1.059）h; Cmax, was （0.795±0.187） ng/mL, （ 1.444±0.245）ng/mL; t1/2 was （ 11.716± 2.005） h, （ 10.62±2.06）h; AUC0-48 was （11.213±4.042） rig. h/mL, （ 18.80 ± 6.98） ng· h/mL. Conclusion： The method is shown to be highly sensitive, accurate and of less interference. It is suitable for pharmaeokinetie study of aztadine.

关 键 词：阿扎他定 LC-MS—MS 药动学 

分 类 号：R969.1[医药卫生—药理学]