Bhattacharya A, Ghosal S K
Department of Pharmaceutical Sciences, Dibrugarh University, India.
Boll Chim Farm. 2000 Jul-Aug;139(4):177-81.
Permeation kinetics for ketotifen fumarate from transdermal system through hairless mice skin and hog skin have been reported. However, permeation of ketotifen fumarate through human skin is not available till date. In view of the above, permeation profile and related kinetic parameters of ketotifen fumarate alone and in presence of three compatible enhancers namely Myristic acid isopropyl ester, Palmitic acid propyl ester and Lauric acid propyl ester through normal and delipidized human cadaver have been reported in the present study. The observed permeability flux, permeation coefficient and epidermal partition coefficient through 50% dried human cadaver epidermis were found to increase in presence of the three enhancers, amongst which the effect was found to be maximum with Myristic acid isopropyl ester. The more pronounced enhancing effect of Myristic acid isopropyl ester regarding permeability flux, permeation coefficient, epidermal partition coefficient and diffusion coefficient was attributed with solubility parameter being nearer to the skin lipid solubility parameter and probably due to its passage across the skin barrier through the lipid pathway.
已报道了富马酸酮替芬从透皮系统透过无毛小鼠皮肤和猪皮肤的渗透动力学。然而，迄今为止，富马酸酮替芬透过人体皮肤的渗透情况尚无报道。鉴于此，本研究报道了富马酸酮替芬单独以及在三种相容性促进剂（即肉豆蔻酸异丙酯、棕榈酸丙酯和月桂酸丙酯）存在的情况下，透过正常和去脂人体尸体皮肤的渗透情况及相关动力学参数。发现在三种促进剂存在的情况下，通过50%干燥人体尸体表皮的观察到的渗透通量、渗透系数和表皮分配系数会增加，其中肉豆蔻酸异丙酯的效果最为显著。肉豆蔻酸异丙酯在渗透通量、渗透系数、表皮分配系数和扩散系数方面具有更显著的促进作用，这归因于其溶解度参数更接近皮肤脂质溶解度参数，并且可能是由于它通过脂质途径穿过皮肤屏障。
