Lien E J, Wang P H
J Pharm Sci. 1980 Jun;69(6):648-50. doi: 10.1002/jps.2600690610.
The effect of molecular weight on drug diffusion and drug action has been described based on the relation D = (RT/6 pi eta N) (cube root of (4 pi N divided by 3M nu-), an inverse relation between the clearance of drugs through artificial membranes and molecular weights, and apparent correlations between log (l/dose) and log mol. wt. for various central nervous system-acting drugs, anticancer drugs, and water-soluble vitamins. In situ rat jejunum permeability data of various drugs were correlated with log P (octanol-buffer) and log mol. wt. A parabolic equation of log P combined with log mol. wt. proposed previously was shown to give significant correlations for hydrolysis data of amides and antifungal data of amines. This model is mathematically simpler and easier to interpret than the more complex curvilinear and bilinear models.
基于关系式(D = (RT/6\pi\eta N)\sqrt[3]{(4\pi N / 3M\nu -)})，描述了分子量对药物扩散和药物作用的影响，该关系式表明药物通过人工膜的清除率与分子量呈反比关系，并且各种中枢神经系统作用药物、抗癌药物和水溶性维生素的对数（(1/剂量)）与对数分子量之间存在明显的相关性。各种药物在大鼠空肠原位渗透数据与对数(P)（辛醇 - 缓冲液）和对数分子量相关。先前提出的对数(P)与对数分子量相结合的抛物线方程被证明对于酰胺的水解数据和胺的抗真菌数据具有显著的相关性。该模型在数学上比更复杂的曲线和双线性模型更简单且更易于解释。
