摘要
将毛细管区带电泳／前沿分析技术用于测定碱性药物ｖｅｒａｐａｍｉｌ（ＶＥＲ）和ｐｒｏｐｒａｎｏｌｏｌ（ＰＲＯ）与人血清白蛋白（ＨＳＡ）平衡体系中结合参数的研究。通过压力进样将药物白蛋白混合液引入石英毛细管电泳柱（３２ｃｍ×５０μｍｉ．ｄ．，聚丙烯酰胺涂渍柱），在ｐＨ值为７．４、离子强度为０．１７的磷酸缓冲液及运行电压为１０ｋＶ的条件下，未结合的碱性药物的浓度可以通过电泳平台峰的高度定量，并且具有良好的线性关系（相关系数ｒ＝０．９９９）。在数据处理过程中成功的采用非线性回归、Ｓｃａｔｃｈａｒｄ方程和Ｋｌｏｔｚ方程３种评价方法，得到了一致的结果。得到的ＶＥＲ和ＰＲＯ与ＨＳＡ的结合参数：结合位点分别是１．２１～１．３０和０．５４～０．６２。
A CZE/FA method was applied to the study of association parameters of basic drugs, verapamil (VER) and propranolol (PRO), to human serum albumin (HSA) under drug HSA association equilibria. After the direct hydrodynamic injection of a drug HSA mixed solution into a coated capillary (effective length, 32 cm; 50 μm i.d.), the basic drug is eluted as a zonal peak with a plateau region under condition of phosphate buffer (pH 7.4, ionic strength=0.17) at 10 kV running voltage. The unbound concentration of drug can be determined from the plateau peak height with good linear response, r=0.999 for both VER(n=6) and PRO(n=8), respectively. Six VER HSA solutions (containing 50 175 μmol/L of VER and 450 325 μmol/L of HSA) and eight PRO HSA solutions (containing 50 400 μmol/L of VER and 450 100 μmol/L of HSA) were investigated. Three analytical methods were used for the present CZE/FA system including Scatchard, Klotz and non linear regression analyses. The estimated association parameters were as follows: the numbers of HSA binding site n for VER were over 1.21(0.04) 1.30(0.09), binding constant, K, was between 1 690(130) and 1 790(70). Whereas for PRO, n=0.54(0.04) 0.62(0.03), and K=1 390(70) 1 690(180) . The data deduced from these three analyses agreed well with each other.
出处
《色谱》
CAS
CSCD
北大核心
1999年第1期58-60,共3页
Chinese Journal of Chromatography
基金
国家自然科学重点基金
交通部基金
关键词
VER
PRO
CZE
碱性药物
人血清白蛋白
结合参数
capillary electrophoresis, frontal analysis, basic drugs, human serum albumin, association parameter
