间尼索地平对映体的大鼠在体肠吸收动力学  

Absorption Kinetics of m-Nisoldipine Enantiomers in Rat's Intestines in situ

作　　者：李敏[1,2] 王春英[1] 孔德志[1] 段坤峰[1] 张兰桐[1] 

机构地区：[1]河北医科大学药学院药物分析教研室,河北石家庄050017 [2]华北煤炭医学院附属医院药剂科,河北唐山063000

出　　处：《中国医药工业杂志》2010年第12期918-921,共4页Chinese Journal of Pharmaceuticals

基　　金：国家自然科学基金项目(30840098);河北省自然科学基金资助项目(C2008001073)

摘　　要：建立HPLC-DAD法测定肠循环液中的间尼索地平,探讨S型和R型间尼索地平在大鼠各肠段的吸收动力学特征,考察药物浓度、pH和吐温-80浓度对药物肠吸收的影响。采用大鼠在体小肠回流装置,使用C_(18)色谱柱,以乙腈-1.0%磷酸(62∶38)为流动相,检测波长353 nm。结果显示间尼索地平对映体在1～80μg/ml浓度范围内与吸收量的线性关系良好,吸收速率常数K_a基本保持不变;各肠段的吸收速率无显著性差异。全肠段吸收呈现一级动力学过程,吸收机制为被动扩散。An HPLC-DAD method was established for the determination of m-nisoldipine enantiomers in the circulation solution of intestine.The absorption kinetics of m-nisoldipine enantiomers at different intestine segments of rats and the influence of the drug concentration,pH and Tween-80 on the absorption kinetics were also investigated.The intestine in rats was cannulated for in situ recirculation.A C_（18） column was used with the mobile phase of acetonitrile- 1.0%phosphoric acid（62：38） at the detection wavelength of 353 nm.The calibration curve of m-nisoldipine enantiomers was linear in the concentration range of 1 - 80μg/ml.The absorption of m-nisoldipine enantiomers in rat＇s intestine was a first-order process with the passive diffusion mechanism.m-Nisoldipine enantiomers can be absorbed in whole intestinal segments.

关 键 词：间尼索地平 对映体 高效液相色谱 肠吸收动力学 吸收速率常数 

分 类 号：R917[医药卫生—药物分析学]