Shin Sang Chul, Lee Hyun Jin
College of Pharmacy, Chonnam National University, Kwangju, South Korea.
Eur J Pharm Biopharm. 2002 Nov;54(3):325-8. doi: 10.1016/s0939-6411(02)00088-7.
Triprolidine-containing matrix was fabricated with ethylene-vinyl acetate (EVA) copolymer to control the release of the drug. The permeation rate of triprolidine in the stripped skin was greatly larger than that in the whole skin. Thus it showed that the stratum corneum acts as a barrier of skin permeation. The effect of penetration enhancer and stripping of skin on the permeation of triprolidine through the excised mouse skin was studied. Penetrating enhancers showed increased flux probably due to the enhancing effect on the skin barrier, the stratum corneum. Among enhancers used such as glycols, fatty acids and non-ionic surfactants, polyoxyethylene-2-oleyl ether showed the best enhancement. The permeability of triprolidine was markedly increased with stripping of the mouse skin to remove the stratum corneum that acts as a barrier of skin permeation. For the controlling transdermal delivery of triprolidine, the application of EVA membrane containing permeation enhancer could be useful in the development of transdermal drug delivery system.
用乙烯-醋酸乙烯酯(EVA)共聚物制备了含曲普利啶的基质,以控制药物释放。曲普利啶在剥离皮肤中的渗透速率远大于在完整皮肤中的渗透速率。因此表明角质层起到了皮肤渗透屏障的作用。研究了渗透促进剂和皮肤剥离对曲普利啶透过离体小鼠皮肤渗透的影响。渗透促进剂显示通量增加,可能是由于对皮肤屏障角质层的增强作用。在所使用的促进剂如二醇、脂肪酸和非离子表面活性剂中,聚氧乙烯-2-油基醚显示出最佳的增强效果。去除作为皮肤渗透屏障的角质层后,曲普利啶的渗透性随小鼠皮肤的剥离而显著增加。对于曲普利啶透皮给药的控制,含有渗透促进剂的EVA膜的应用可能有助于透皮给药系统的开发。