Effect of albumin on the absorption of phenol red, bromphenol blue and bromosulphonphthalein as model drugs from the liver surface membrane in rats.
Effect of albumin on the absorption of phenol red, bromphenol blue and bromosulphonphthalein as model drugs from the liver surface membrane in rats.
复制标题
白蛋白对大鼠肝表面膜吸收模型药物酚红、溴酚蓝和溴磺酞的影响。
DOI：
10.1248/bpb.18.1548
复制
发表时间：
1995
影响因子：
2
通讯作者：
J. Nakamura
中科院分区：
文献类型：
--
作者：
K. Nishida;N. Sato;H. Sasaki;J. Nakamura
以苯酚红、溴酚蓝和溴磺酞为模型药物，研究了牛血清白蛋白（BSA）对大鼠肝表面药物吸收的影响。在BSA浓度为0.1—10% （w/v）时，模型药物（磷酸盐缓冲液中为3mg /ml）与BSA的结合率变化很大。将模型药物（3mg /ml × 0.1 ml）加或不加牛血清白蛋白，通过圆柱形玻璃细胞（直径9 mm，面积0.64 cm2）在体内施加于大鼠肝脏表面。模型药物在6h时从大鼠肝表面的吸收比（以玻璃细胞的回收量计算）随着BSA浓度的增加而降低。模型药物的胆道恢复也有类似的趋势。三种有机阴离子中，溴磺酞对牛血清白蛋白的结合活性最高，其吸收比明显降低。因此，蛋白质结合似乎是药物从肝脏表面吸收的一个重要因素。
The effect of bovine serum albumin (BSA) on drug absorption from the liver surface in rats was examined by using three organic anions (phenol red, bromphenol blue and bromosulphonphthalein) as model drugs which have a high affinity for albumin. The binding ratio of the model drugs (3 mg/ml in phosphate buffer) to BSA varied widely at a BSA concentration of 0.1--10% (w/v). The model drugs (3 mg/ml x 0.1 ml) with or without BSA were applied to the rat liver surface in vivo employing a cylindrical glass cell (i.d. 9 mm, area 0.64 cm2). The absorption ratios of the model drugs from the rat liver surface at 6h, calculated from the amount recovered from the glass cell, decreased with an increase in BSA concentration. A similar trend was observed with biliary recovery of the model drugs. A marked reduction in the absorption ratio was seen with bromosulphonphthalein, which has the highest binding activity to BSA among the three organic anions. Accordingly, protein binding appears to be a significant factor with respect to the drug absorption from the liver surface.