摘要
目的:建立LC/MS/MS法测定人血浆中地洛他定浓度,并研究地洛他定在中国男性健康人体内的药代动力学。方法:采用LC/MS/MS（APCI源）测定地洛他定的血浆浓度,并计算药代动力学参数。结果:地洛他定的定量限为0.2μg·L-1,该法的日内及日间精密度（RSD）均小于10％,准确度（RE）在±3％范围内。20名中国男性健康受试者口服单剂量20mg地洛他定片后,主要药供代动力学参数分别为:tmax为（2.2±0.7）h,t1/2为（16.1±4.6）h,Cmax为（15.1±6.7）μg·L-1,AUC0-48h为（176.4±70.2）μg·h·L-1,Ke为（0.046±0.011）h-1。结论:该法操作简便、快速、灵敏,成功用于测定血浆中地洛他定浓度;并首次报道了地洛他定在中国男性健康人体内的药代动力学参数。
OBJECTIVE: To develop a LC/MS/MS method for quantifying desloratadine in human plasma and to study pharmacokinetics of desloratadine in healthy male Chinese volunteers. METHODS: The concentrations of desloratadine were determined by LC/MS/MS with APCI and the pharmacokinetic parameters were calculated. RESULTS: The lower limit of quantitation was 0.2μg·L-1. The intra-and inter-run precision was measured to be below 10%. The was less than 3% for the analyte. After an oral administration of 20 mg desloratadine to 20 volunteers,the main pharmacokinetic parameters of desloratadine were as follows: tmax (2.2±0.7) h, t1/2 was (16.1±4.6) h, Cmax was (15.1±6.7) μg·L-1,AUC0-48h was 76.4±70.2) μg·h·L-11 and Ke was (0.046±0.011) h-1 . CONCLUSION: The method is shown to be convenient, accurate and robust, suitable for determination of desloratadine in human plasma and pharmacokinetic studies of desloratadine.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2002年第3期211-214,共4页
The Chinese Journal of Clinical Pharmacology
基金
国家自然科学基金资助项目(No.39930180)
