Ghosh B, Reddy L H
Department of Pharmaceutical Technology, V. L. College of Pharmacy, Raichur, India.
Indian J Exp Biol. 2001 Jul;39(7):710-4.
Studies were carried out to establish a correlation of skin permeability with physicochemical parameters using five antihypertensive drugs. In vitro skin permeation was carried out in vertical type diffusion cells. When steady-state fluxes of the drugs were correlated with physicochemical properties, good correlation was obtained with the reciprocal of melting point. Weak correlation was obtained with partition coefficient, molecular weight and solubility. However skin permeability versus solubility profiles revealed an interesting trend. The initial permeation rates of the poorly water soluble drugs, prazosin hydrochloride and reserpine were higher than their steady-state fluxes and moderately water soluble drug atenolol showed more or less similar permeation throughout the entire span of the study. This trend changed gradually and reversed completely in the highly water soluble drug diltiazem hydrochloride. The study suggests that drug derivatives of low melting point and good aqueous solubility could be favorable candidates for transdermal delivery.
使用五种抗高血压药物进行了研究，以建立皮肤渗透性与物理化学参数之间的相关性。在垂直型扩散池中进行体外皮肤渗透实验。当将药物的稳态通量与物理化学性质相关联时，与熔点的倒数获得了良好的相关性。与分配系数、分子量和溶解度的相关性较弱。然而，皮肤渗透性与溶解度曲线显示出一个有趣的趋势。水溶性差的药物盐酸哌唑嗪和利血平的初始渗透速率高于其稳态通量，而中等水溶性药物阿替洛尔在整个研究过程中显示出或多或少相似的渗透率。在高水溶性药物盐酸地尔硫䓬中，这种趋势逐渐改变并完全逆转。该研究表明，低熔点和良好水溶性的药物衍生物可能是经皮给药的有利候选物。
