Liang D
Zhejiang Branch, Hangzhou.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao. 1990 Aug;12(4):262-9.
A series of 13 p-aminobenzoate esters were selected as model drugs to study correlations between HPLC retention parameters and percutaneous rate. The octanol/water partition coefficient and solubility of these compounds were determined and their permeation through rat skin was measured using a Franz diffusion cell. Capacity factor and retention index were used as HPLC retention parameters and calculated from their retention times. The results indicate that for the p-aminobenzoate esters studied, the capacity factors and retention indices obtained in our experimental conditions are indicators of relative lipophilicity of drugs and can be used to predict their steady-state fluxes and permeation coefficients by using the Hansch equation. They are easy to obtain and reproducible enough to substitute for the more laborious and inaccurate partition coefficient values.
选择了一系列13种对氨基苯甲酸酯作为模型药物，以研究高效液相色谱保留参数与经皮速率之间的相关性。测定了这些化合物的正辛醇/水分配系数和溶解度，并使用Franz扩散池测量了它们在大鼠皮肤上的渗透情况。容量因子和保留指数用作高效液相色谱保留参数，并根据它们的保留时间进行计算。结果表明，对于所研究的对氨基苯甲酸酯，在我们的实验条件下获得的容量因子和保留指数是药物相对亲脂性的指标，并且可以通过使用Hansch方程来预测它们的稳态通量和渗透系数。它们易于获得且具有足够的重现性，足以替代更费力且不准确的分配系数值。
