【摘要】 采用水平双室扩散池,以离体鼠皮为透过屏障,考察介质和有机酸对来曲唑体外经皮透过性的影响。在肉豆蔻酸异丙酯(IPM)中加入乙醇后能明显地增加来曲唑的经皮透过量,尤其以含有20%(w/w)乙醇的IPM混合溶液促进作用最为显著。在此溶液系统中,加入的有机酸和来曲唑形成了复合物明显地增加了来曲唑的经皮透过性。由于加入有机酸的结构不同,因此其对来曲唑经皮通透具有不同的促进作用。本实验的结果表明在含有20%乙醇的IPM溶液系统中加入有机酸是促进来曲唑经皮透过性更为有效的方法。更多还原

【Abstract】 The purpose of this study was to investigate the effects of vehicles and organic acids on the in vitro permeation of letrozole across rat skin. Permeation experiments were carried out with 2-chamber diffusion cells through rat skin. The binary solvent mixture of ethanol and isopropyl myristate (IPM) could markedly enhance the cumulative penetrated amount of letrozole after 8 h (Q 8 ) compared with IPM alone, especially the IPM system containing 20% (w/w) ethanol. Surprisingly, the use of complexation with organic acids facilitated skin permeation of letrozole in the IPM–ethanol (20%, w/w) system. Due to different structures of tested organic acids, their effects on the penetration of letrozole were different. This study showed that the addition of an organic acid in the IPM–ethanol (20%, w/w) system was a promising approach to enhance the skin permeability of letrozole.更多还原