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经方差分析无显着差异,用单位体重的曲线下面积对剂量进行线性回归存在显着正相关。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。
Abstract:
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=0.37L/kg,Tα/2=6.4min,Tβ/2=84.1min,AUC=94.1mg·min/L,CL=0.65L/(kg·h).No statistically significant diference was found in C1 and Tβ/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.