Chien Y W, Lambert H J, Lin T K
J Pharm Sci. 1975 Jun;64(6):961-6. doi: 10.1002/jps.2600640614.
The extent of plasma binding and the partition coefficient of disopyramide and 20 disopyramide derivatives were determined. Structural variations on the four functional groups around the tetrahedral carbon in the disopyramide molecule was found to influence both parameters to varying degrees. Three linear equations were developed to correlate the observed effects, depending on the type of chemical modification. The linear correlation between drug-plasma interaction and lipophilic character was analyzed theoretically. A simple model was derived to relate quantitatively the variation in the extent of plasma binding to the change in lipophilicity of disopyramide derivatives.
测定了丙吡胺及其20种衍生物的血浆结合程度和分配系数。发现丙吡胺分子中四面体碳周围四个官能团的结构变化对这两个参数均有不同程度的影响。根据化学修饰的类型，建立了三个线性方程来关联观察到的效应。从理论上分析了药物与血浆相互作用和脂溶性之间的线性关系。推导了一个简单的模型，以定量地将血浆结合程度的变化与丙吡胺衍生物亲脂性的变化联系起来。
