Fang J, Wang R, Huang Y, Wu P C, Tsai Y
School of Pharmacy, Kaohsiung Medical University, 100 Shih-Chuan 1st Road, Kaohsiung, Taiwan.
Biol Pharm Bull. 2000 Nov;23(11):1357-62. doi: 10.1248/bpb.23.1357.
The in vitro permeation of three diclofenac salts--diclofenac sodium (DFS), diclofenac potassium (DFP) and diclofenac diethylammonium (DFD)-across skin by both passive and iontophoretic transport were investigated. Various skin types were used as the barriers to elucidate the mechanism controlling transdermal delivery of diclofenac salts. The importance of the intercellular (paracellular) route for both DFS and DFP in passive permeation was elucidated. The transfollicular route constitutes an important permeation pathway for DFS but not for DFP. The route and mechanism for transdermal iontophoresis of DFD across the skin was somewhat different to that of the other salts. Hair follicles may be a more important pathway for DFD than for DFS and DFP under iontophoresis, while the intercellular lipid pathway showed the opposite result. Combination of iontophoresis and a penetration enhancer, cardamom oil, did not show a synergistic effect on diclofenac salt permeation. The results of this investigation suggest that the transdermal mechanism and the route of diclofenac salt uptake via passive and iontophoretic transport can be affected by their counterions.
研究了双氯芬酸钠（DFS）、双氯芬酸钾（DFP）和双氯芬酸二乙胺盐（DFD）这三种双氯芬酸盐通过被动和离子导入转运在体外透过皮肤的情况。使用了多种皮肤类型作为屏障，以阐明控制双氯芬酸盐透皮给药的机制。阐明了细胞间（旁细胞）途径在DFS和DFP被动渗透中的重要性。经毛囊途径是DFS的重要渗透途径，但不是DFP的重要渗透途径。DFD经皮肤离子导入的途径和机制与其他盐类有所不同。在离子导入条件下，毛囊对DFD可能比对DFS和DFP是更重要的途径，而细胞间脂质途径则显示出相反的结果。离子导入与渗透促进剂小豆蔻油联合使用，对双氯芬酸盐的渗透未显示出协同作用。本研究结果表明，双氯芬酸盐通过被动和离子导入转运的透皮机制及摄取途径会受到其抗衡离子的影响。
