Dias M, Hadgraft J, Lane M E
Department of Pharmaceutics, School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, United Kingdom.
Int J Pharm. 2007 Aug 1;340(1-2):65-70. doi: 10.1016/j.ijpharm.2007.03.030. Epub 2007 Mar 30.
The relative importance of solubility parameters and other solvent properties on membrane diffusion processes has not been fully elucidated in the literature. Previously, we have studied the effect of different vehicles on the permeation of caffeine, benzoic acid (BA) and salicylic acid (SA) through silicone membranes. The present paper investigates diffusion of the selected permeants from different saturated solutions through human epidermis. The permeation of caffeine was strongly affected by the vehicle chosen and the maximum enhancement observed for the permeation of caffeine was 288-fold. A maximum of 12-fold enhancement in the flux was observed for the permeation of SA and a maximum of 10-fold enhancement was observed for the permeation of BA. The diffusion profiles obtained for SA in the different solvents were very similar when compared with those obtained for BA but the permeation rates were higher for BA than for SA. This similarity results from the similar chemical structure and lipophilicity.
溶解度参数和其他溶剂性质对膜扩散过程的相对重要性在文献中尚未得到充分阐明。此前,我们研究了不同载体对咖啡因、苯甲酸(BA)和水杨酸(SA)透过硅膜渗透的影响。本文研究了所选渗透物从不同饱和溶液通过人体表皮的扩散情况。咖啡因的渗透受到所选载体的强烈影响,观察到咖啡因渗透的最大增强倍数为288倍。SA渗透通量的最大增强倍数为12倍,BA渗透通量的最大增强倍数为10倍。与BA相比,SA在不同溶剂中获得的扩散曲线非常相似,但BA的渗透速率高于SA。这种相似性源于相似的化学结构和亲脂性。