Determination of Loratadine in Human Plasma by High Performance Liquid Chromatography-Electrospray Mass Spectrometry and Studies on Its Pharmacokinetics and Relative Bioavailability  

液质联用法测定人血浆中氯雷他定的浓度及其药动学研究(英文)

作　　者：陈钧[1] 高科攀[1] 史振祺[1] 陆伟[1] 蒋新国[1] 荣征星[2] 黄霞[2] 陈红专[2] 

机构地区：[1]复旦大学药学院药剂学教研室,上海200032 [2]上海第二医科大学国家药品临床研究基地,上海200025

出　　处：《Journal of Chinese Pharmaceutical Sciences》2002年第4期137-141,共5页中国药学（英文版）

摘　　要：A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined by mass detector. The calibration curve of loratadine was linear within the range of 0.4～100 ng·mL -1 with r=0.9995 . The recovery of this method was within 95%～104%, within day and between day RSD were less than 12%. To study the pharmacokinetics and relative bioavailability of loratadine tablets, two formulations of loratadine tablets were given to 18 healthy male volunteers according to a randomized 2 way cross over design. The C max , AUC 0 t and T max values of the two formulations were 51.89±20.18 ng·mL -1 and 52.48±22.35 ng·mL -1 ; 140.75±88.42 ng·h·mL -1 and 147.24±92.33 ng·h·mL -1 ; 0.81±0.35 h and 0.81±0.27 h respectively. Results from statistic analysis showed that there were no significant difference between the C max , AUC 0-t and T max values of the two formulations. The relative bioavailability of tablets I with respect to tablets II was 97%±13% from the AUC 0 t measurement. Bioequivalance was observed between the two tablets.本文首次建立了测定人血浆中氯雷他定的液质联用方法。本方法采用有机溶剂提取药物后由ODS柱分离 ,质谱检测器测定。该方法的线性范围为 0 .4～ 10 0ng·mL-1,(r=0 .9995 ) ,方法回收率在 95 %～ 10 4 %之间 ,日内和日间精密度都小于 12 %。采用自身对照交叉给药方式 ,单剂量分别给予 18名男性健康志愿者两种国产氯雷他定片 4 0mg ,其主要药动学参数Cmax,AUC0 -t和Tmax分别为 :5 1.89± 2 0 .18ng·mL-1和 5 2 .4 8± 2 2 .35ng·mL-1;14 0 .75± 88.4 2ng·h·mL-1和 14 7.2 4± 92 .33ng·h·mL-1;0 .81± 0 .35h和 0 .81± 0 .2 7h。统计学结果表明 :两种制剂间的主要动力学参数无明显差异 ,为生物等效制剂 ,其相对生物利用度为 97%± 13%。

关 键 词：LORATADINE HPLC  MS PHARMACOKINETICS BIOAVAILABILITY 

分 类 号：R969[医药卫生—药理学]