间硝苯地平在兔体内的药物动力学  

Pharmacokinetics of m-nifedipine in rabbits after intravenous injection

作　　者：王勇 马骏[1,2] 

机构地区：[1]解放军第280医院药械科 [2]兰州军区总医院药材科

出　　处：《药学实践杂志》1999年第2期95-96,共2页Journal of Pharmaceutical Practice

摘　　要：目的：研究间硝苯地平剂量效应的药代动力学。方法：兔被随机分成３组，分别静脉注射高、中、低（０５，１，２ｍｇ／ｋｇ）３种剂量的间硝苯地平，用ＨＰＬＣ法测定血浆药物浓度。结果：间硝苯地平的血药浓度和时间数据经拟合均符合二室模型，主要药动学参数如下（以剂量１ｍｇ／ｋｇ为例）：Ｖｄ＝０３７Ｌ／ｋｇ，Ｔα／２＝６４ｍｉｎ，Ｔβ／２＝８４１ｍｉｎ，ＡＵＣ＝９４１ｍｇ·ｍｉｎ／Ｌ，ＣＬ＝０６５Ｌ／（ｋｇ·ｈ）。各剂量组间的ＣＬ，Ｔβ／２经方差分析无显著差异，用单位体重的曲线下面积对剂量进行线性回归存在显著正相关。结论：间硝苯地平分布广，消除也迅速；在剂量０５～２ｍｇ／ｋｇ范围内消除动力学呈非剂量依赖性关系。OBJECTIVE: To study the dose effects on pharmacokinetics of m-Nif. METHODS: 15 rabbits were divided into 3 groups receiving iv m-Ni f 05,1,and 2 mg/kg Plasma levels of m-Nif were determined with HPLC method. RESULTS: The concentration-time data were fitted with 2-compartment model.The parameters were after iv l mg/kg:Vd=(0370.10) L/kg,T/2=(6.42.9)min,T/2=(84.122.0)min,AUC=(94.116.2)mgmin/L,CL=(0.650.13)L/(kgh).No statistically significant diference was found in C1and T/2 between 3 dose groups.AUC (standardized to body weight)was correlated with doses. CONCLUSION: m-Nif was distributed widely and eliminated at a fairly rapid rate in the rabbits.No dose-dependent pharmacokinetics was found after iv m-Nif 0.52mg/kg.

关 键 词：间硝苯地平 高压液相色谱法 药物动力学 

分 类 号：R972.3[医药卫生—药品] R969.1[医药卫生—药学]