Liang W Q, Lin W
Department of Pharmaceutics, Zhejiang Medical University, Hangzhou.
Yao Xue Xue Bao. 1992;27(9):684-9.
A series of 8 p-aminobenzoate esters were selected as model drugs to study the effect of molecular volume and partition coefficient on percutaneous absorption. The octanol/water partition coefficient and solubility of these compounds were determined and their penetration rate through rat skin in vitro was measured using a Keshany-Chien diffusion cell. The results showed that when the molecular volume was increased the permeation coefficient was decreased. However, when the partition coefficient was increased, the permeation coefficient was increased at first and then reached a plateau. The mathematical formula has been derived from a bi-layer diffusion model to show how the molecular volume and the partition coefficient influence the permeation coefficient. The formula could be used to estimate the permeation coefficient of drug through skin.
选择了一系列8种对氨基苯甲酸酯作为模型药物，以研究分子体积和分配系数对经皮吸收的影响。测定了这些化合物的正辛醇/水分配系数和溶解度，并使用Keshany-Chien扩散池测量了它们在体外透过大鼠皮肤的渗透率。结果表明，当分子体积增大时，渗透系数降低。然而，当分配系数增大时，渗透系数起初增大，然后达到平稳状态。已从双层扩散模型推导出数学公式，以显示分子体积和分配系数如何影响渗透系数。该公式可用于估算药物透过皮肤的渗透系数。
