In vitro characterization of sodium glycocholate binding to cholestyramine resin.
In vitro characterization of sodium glycocholate binding to cholestyramine resin.
复制标题
甘胆酸钠与考来烯胺树脂结合的体外表征。
DOI：
10.1002/jps.2600840114
复制
发表时间：
1995
影响因子：
3.8
通讯作者：
Amidon,GL
中科院分区：
文献类型：
--
作者：
Polli,JE;Amidon,GL
胆酸隔离剂中的胆胺树脂，与肠腔中的胆盐结合，增加胆盐的粪便排泄，从而降低血清胆固醇。为了更好地了解胆甾胺的低活效性，在体外平衡结合研究、吸水研究和树脂容量测量中使用胆甾胺和胆盐糖胆酸钠。平衡结合和水吸附研究需要将胆碱（1.0 - 20mg /mL）与糖胆酸盐阴离子浓度（0.20-16.5 mM）和氯离子浓度（15-150 mM）不同的溶液进行平衡。树脂对糖胆酸盐的实际比容量低于氯离子的实际比容量。这一差异表明，坚硬、笨重的胆盐在10%的树脂离子生成位点被孔排除。通过测量游离糖胆酸盐和氯阴离子浓度，提出了容量校正摩尔选择系数KCl - GC -的基本参数来描述潜在的结合现象；KCl‐GC−的范围从9.8（±0.7）到18.6（±0.2），取决于游离氯化物浓度的平方。容量校正后的摩尔选择系数大于糖胆酸的摩尔选择系数。一种更简单的计算容量校正摩尔选择系数的方法所需的数据更少，其结果与更严格的方法相似（r2= 0.955）。
Cholestyramine resin in a bile acid sequestrant which binds with bile salts in the intestinal lumen to increase the fecal excretion of bile salts and, thus, lower blood serum cholesterol. In order to gain a better understanding of the lowin vivopotency of cholestyramine,in vitroequilibrium binding studies, water sorption studies, and resin capacity measurements were performed using cholestyramine and the bile salt sodium glycocholate. Equilibrium binding and water sorption studies entailed equilibrating cholestyramine (1.0–20 mg/mL) with solutions which varied in glycocholate anion concentration (0.20–16.5 mM) and chloride anion concentration (15–150 mM). The resin's practical specific capacity for glycocholate was lower than the practical specific capacity for chloride. This difference suggests that the rigid, bulky bile salt was pore excluded from 10% of the resin's ionogentic sites. A fundamental parameter called the capacity‐corrected molar selectivity coefficient,KCl‐GC−, was postulated to describe the underlying binding phenomena and was determined by measuring the free glycocholate and chloride anion concentrations;KCl‐GC− ranged from 9.8 (±0.7) to 18.6 (±0.2) and depended on the square of the free chloride concentration. The capacity‐corrected molar selectivity coefficient was larger than the molar selectivity coefficient due to pore exclusion of glycocholate. A more simple method to calculate the capacity‐corrected molar selectivity coefficient which required less data gave similar values to the more rigorous method (r2= 0.955).