摘要
目的:研究氯雷他定血浆浓度测定方法及其在健康人体内的药动学。方法:18名健康男性志愿者单剂量口服氯雷他定片,在设计的时间点取静脉血,采用高效液相色谱-质谱法(HPLC-MS)测定血药浓度。药动学参数采用DAS程序计算。结果:单次口服20mg氯雷他定片后的主要药动学参数AUC_0～t、AUC_0～∞、C_(max)、t_(max)、t_(1/2)分别为(32.26±21.54)μg/(L·h)、(37.18±22.53)μg/(L·h)、(12.00±7.50)μg/L、1.56±0.70)h和(11.15±19.66)h。结论:本法适用于快速准确及高灵敏地警测定血浆中的氯雷他定,其在研究人体内口服吸收较快,个体间差异较大,约1.5h达血药浓度峰值,平均消除半衰期为11h。
Objective ：To develop a sensitive and specific LC/MS method for direct determination of loratadine in human plasma and study the pharmacokineties of loratadine. Methods：After a single dose oral administration of loratadine 20 mg to 18 healthy Chinese male volunteers, the plasma concentrations of loratadine were determined. Loratadine and internal standard diazepam were extracted from plasma using liquid-liquid extraction. Plasma concentration of Ioratadine was determined by HPLC-MS, and calculated the pharmacokinetic parameters. Results：The linear calibration curves were obtained in the coneent ration range of 0. 25 - 40. 0μg · L ^- 1 The limit of quantity was 0. 25μg · L ^- 1 . Pharmacokinetic parameters of loratadine was obtained as follows ： AUC0 - t was （ 32. 26 ± 21.54 ） μg/（ L · h）, AUC0 - ∞ was （ 37. 18 ± 22. 53 ） μg/（ L · h） ,Cmax was（ 12.00 ±7. 50） μg/L,tmax was（ 1.56 ±0. 70） h,t1/2was（ 11.15 ± 19. 66） h. Conclusions：The method is proved to be suitable for pharmacokinetic evaluation of loratadine.
出处
《中国医药导刊》
2009年第4期656-658,共3页
Chinese Journal of Medicinal Guide
