摘要
目的:研究间硝苯地平剂量效应的药代动力学。方法:兔被随机分成三组,分别静脉注射高、中、低(0.5,1,2mg·kg^(-1))三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^(-1)为例):V_d=0.37 L·kg^(-1),T_(1/2α)=6.4min,T_(1/2β)=84.1min,AUC=94.1mg·min·L^(-1),Cl=0.65L·kg^(-1)·h^(-1)。各剂量组间的Cl,T_(1/2β)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^(-1)范围内消除动力学呈非剂量依赖性关系。
AIM: To study the dose effects on pharmacokinetics of m-Nif. METHODS: Fifteen rabbits were divided into 3 groups receiving iv m-Nif 0.5, 1, and 2 mg ·kg-1 . Plasma levels of m-Nif were determined with HPLC method. RESULTS: The concentration-time data were fitted with 2-compartment model. After iv 1 mg · kg -1, the parameters were: Vd = 0.37 ±0.10 L·kg-1, T1/2a = 6.4±2.9 min,
T1/2b = 84± 22 min, AUC= 94 ± 16 mg·min·L-1,
Cl = 0.65 ± 0.13 L · kg-1 · h-1. No statistically significant difference was found in Cl and T1/2b
between 3 dose groups. AUC ( standardized to body weight) was correlated with doses. CONCLUSIONS : 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 0.5-2 mg·kg-1.
出处
《中国药理学报》
CSCD
1996年第2期109-111,共3页
Acta Pharmacologica Sinica
关键词
间硝苯地平
液相色谱法
药物动力学
兔
m-nifedipine
high pressure liquid chromatography
pharmacokinetics
dihydropyridines
