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间尼索地平在大鼠体内的组织分布、排泄及血浆蛋白结合率的测定

Tissue Distribution and Excretion of m-Nisoldipine in Rats and Its Plasma Protein Binding

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【作者】 王树华; 尚清; 张永健;

【Author】 WANG Shu-Hua1,2, SHANG Qing3 , ZHANG Yong-Jian1*(1.Dept. of Pharmacology, Hebei Medical University, Shijiazhuang 050017; 2. Dept. of Pharmacology, North China Coal Medical College, Tangshan 063000; 3.Pharmic Dept. the People’s Hospital of Hebei Province, Shijiazhuang 050051)

【机构】 河北医科大学药理室; 河北省人民医院药学部; 河北医科大学药理室 河北石家庄050017华北煤炭医学院药理室; 河北唐山063000; 河北石家庄050051; 河北石家庄050017;

【摘要】 建立了HPLC法测定生物样品中间尼索地平的含量,并研究了其在大鼠体内的组织分布、排泄及血浆蛋白结合率等特征。以尼莫地平为内标,样品采用液-液萃取。采用C18柱,流动相为乙腈-20mmol/LKH2PO4溶液(60∶40),检测波长237nm。间尼索地平在2~1000ng/ml范围内,线性关系良好。间尼索地平在大鼠体内分布广泛,经粪便及胆汁的排泄量均较少,而尿中则未检出药物原型,间尼索地平的血浆蛋白结合率达97%以上。

【Abstract】 A HPLC method was established for determination of m-nisoldipine in rats. The tissue distribution and excretion of m-nisoldipine in rats and its plasma protein binding were discussed. Nimodipine was used as internal standard. The samples were extracted by liquid-liquid extraction method. A C18 column was used with the mobile phase of acetonitrile-20mmol/L KH2PO4 solution (60∶40), at the detection wavelength of 237 nm. The calibration curves of m-nisoldipine were linear in the range of 2 - 1000 ng/ml. m-Nisoldipine could be detected in all tissue samples but not been found in urine. The excretions through the faeces and bile were low. Plasma protein binding ratio of m-nisoldipine was over 97%.

【基金】 河北省卫生厅重大攻关课题(编号04002)
  • 【文献出处】 中国医药工业杂志 ,Chinese Journal of Pharmaceuticals , 编辑部邮箱 ,2006年11期
  • 【分类号】R96
  • 【被引频次】17
  • 【下载频次】495
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