Fang J Y, Fang C L, Hong C T, Chen H Y, Lin T Y, Wei H M
Graduate Institute of Pharmaceutical Sciences, Taipei Medical College, 250 Wu-Hsing Street, Taipei, Taiwan.
Eur J Pharm Sci. 2001 Jan;12(3):195-203. doi: 10.1016/s0928-0987(00)00118-4.
The study was conducted in vitro to investigate the changes of indomethacin transdermal permeation pretreated by capsaicin and nonivamide, two compounds chemically similar to Azone. The combined effect of low frequency ultrasound (20 kHz) and enhancers on the indomethacin permeation was also evaluated. The experimental data demonstrated that capsaicin and nonivamide significantly enhanced the flux of indomethacin across nude mouse skin. Enhancement effects of both analogues were very similar and depended predominantly on the concentration tested. Histological examination coupled with visual scores indicated the safety of capsaicin and nonivamide on skin structure. Simultaneous application of ultrasound and enhancers significantly increased skin permeation of indomethacin compared with either ultrasound or enhancers alone. Better effect was obtained by the combination with capsaicin than nonivamide.
本研究在体外进行，以调查辣椒素和壬酰胺（两种与氮酮化学结构相似的化合物）预处理后吲哚美辛经皮渗透的变化。还评估了低频超声（20 kHz）和渗透促进剂对吲哚美辛渗透的联合作用。实验数据表明，辣椒素和壬酰胺显著提高了吲哚美辛透过裸鼠皮肤的通量。两种类似物的增强效果非常相似，且主要取决于所测试的浓度。组织学检查结合视觉评分表明辣椒素和壬酰胺对皮肤结构具有安全性。与单独使用超声或渗透促进剂相比，同时应用超声和渗透促进剂显著增加了吲哚美辛的皮肤渗透。与壬酰胺联合使用相比，与辣椒素联合使用效果更佳。
