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采用离体皮肤扩散等技术研究了5-Fu在人皮肤各层次中的渗透性质和1,8-CN对药物渗透及皮肤热转变的影响。实验表明5-Fu在皮肤各层次中有相近分配系数,但扩散性质不同。角质层、全皮层、脱脂角质层和去角质层全皮扩散系数依次为1.32×10~(-7),1.01×10~(-7),1.37×10~(-6)和54.09×10~(-6)cm~2/h。用1,8-CN处理上述皮肤样品12h后,5-Fu在各组织的分配均减少,角质层和全皮的通透性显著增加(P<0.05),对去脂角质层和去角质层全皮的通透性无明显影响。结合DSC分析证明,角质层是5-Fu经皮渗透的重要屏障,类脂对5-Fu的扩散和1,8-CN的增效具重要意义。
The effects of 5-Fu on the permeation of human skin and the effects of 1,8-CN on drug permeation and skin thermal transition were studied by ex vivo skin diffusion and other techniques. Experiments show that 5-Fu has similar distribution coefficients in different layers of skin, but different diffusion properties. The whole skin diffusivities of the stratum corneum, the whole cortex, the skim stratum corneum and the exfoliation layer were 1.32 × 10 -7, 1.01 × 10 -7, 1.37 × 10 -6 and 54.09 × 10 ~ (-6) cm ~ 2 / h. Treatment of these skin samples with 1,8-CN for 12 h reduced the distribution of 5-Fu in each tissue and increased the permeability of the stratum corneum and whole skin (P <0.05) Permeability of whole skin had no significant effect. Combined with DSC analysis, stratum corneum is an important barrier to 5-Fu transdermal penetration. Lipids are important for the proliferation of 5-Fu and the synergism of 1,8-CN.