高效液相色谱法测定人血浆中尼卡地平及药代动力学参数  

HPLC Determination of Nicardipine in Human Plasma and Its Pharmacokinetic Parameters

作　　者：李克[1] 张昕[1] 赵飞浪[1] 袁倚盛[1] 

机构地区：[1]南京军区南京总医院中心仪器分析室

出　　处：《中国药科大学学报》1998年第3期197-200,共4页Journal of China Pharmaceutical University

摘　　要：建立了反相高效液相色谱法检测正常人口服尼卡地平片剂后的血药浓度。样品经硼酸缓冲液（ｐＨ９０）碱化后，用正己烷正丁醇混合溶剂（１２∶１，Ｖ／Ｖ）提取，以Ｃ１８化学键合硅胶为固定相，乙腈ＫＨ２ＰＯ４缓冲液（００１５ｍｏｌ／Ｌ，ｐＨ＝５５）三乙胺为流动相，尼莫地平为内标，在２３６ｎｍ波长定量检测。血药浓度在５～２００ｎｇ／ｍｌ范围内线性良好，最低检测浓度为２５ｎｇ／ｍｌ。日内（ｎ＝７）及日间（ｎ＝５）测定相对标准偏差分别小于５４％和６４％，血样测定回收率为９２８％１００８％。用本法监测了１０名健康人口服盐酸尼卡地平片剂后不同时间的血药浓度变化，测得血浆中尼卡地平浓度在１６±０３ｈ达到峰值１０９８±３８７ｎｇ／ｍｌ，Ｔ１／２＝５３５±２２８ｈ，血药浓度曲线下面积为３２２１±６９６ｎｇ·ｈ／ｍｌ。A simple and sensitive reversedphase liquid chromatographic method has been developed and validated for the analysis of nicardipine in human plasma and the study of pharmacokinetics of the drug in human body Nicardipine and nimodipine (internal standard) in plasma were extracted with hexanebutanol (12∶1, V/V), and then measured by HPLC using a Hypersil C18 column as stationary phase and a acetonitrile KH2PO4 buffer (0015 mol/L, pH=55)triethylamine as mobile phase Nicardipine was quantified by ultraviolet absorbance at 236 nm The method proved to be linear in the clinical range of 5￣200 ng/ml with a regression coefficient of 09998 The lower limit of detection of nicardipine in plasma was 25 ng/ml Intraday and interday coefficients of variation of assay for nicardipine in plasma were 35 %￣54 % (n=7) and 52 %～64 % (n=5), respectively The recoveries of nicardipine were 928 %～1008 % for plasma The method has been used to determine nicardipine in plasma samples from ten volunteers and provided data on the pharmacokinetics of the drug The results inferred that nicardipine was absorbed rapidly and had a relatively short halflife time in healthy individuals The data obtained was fitted with 3P87 program on computer to study the pharmacokinetics The results showed that the disposition of nicardipine was conformed to a twocompartment open model with Tmax=16±03 h, Cmax=1098±387 ng/ml, T1/2=535±228 h and AUC0→∞=3221±696 ng·h/ml

关 键 词：尼卡地平 高效液相色谱法 药物分析 药物动力学 

分 类 号：R972[医药卫生—药品] R969.1[医药卫生—药学]