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%。
