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采用扩散装置和放射性同位素标记物测定,辅以FTIR和DSC技术,研究了雌二醇(OE)在角质层、去脂角质层、表皮以及活性表皮中的渗透性质和分配性质,分析角质层及其类脂在亲脂性药物经皮渗透中的作用。实验表明角质层是该类药物渗透的屏障,OE在其中的渗透速度受到角质层通透性和药物在角质层分配系数的双重控制,而OE从角质层转运至活性表皮的过程不成为限速因素。角质层的屏障性质仅部分来源于角质层类脂,而角质层细胞膜产生的阻力则是角质层屏障性质的重要组成部分。角质层类脂同时又可能是OE扩散的途径,该类物质通过对亲脂性药物增溶、提高后者在角质层中的分配产生影响。促进剂1,8-桉油精(1,8-CN)对OE的促渗作用也部分地依赖于角质层类脂的存在,通过一种可逆的物理相互作用改变类脂途径的通透性。
The proliferation and distribution properties of estradiol (OE) in the stratum corneum, the stratum corneum, the epidermis and the active epidermis were studied by means of diffusion devices and radioisotope labeling, supplemented with FTIR and DSC techniques. The stratum corneum, The role of lipids in transdermal penetration of lipophilic drugs. Experiments show that the stratum corneum is a barrier to the penetration of such drugs. The penetration speed of OE therein is controlled by both the permeability of the stratum corneum and the distribution coefficient of the drug in the stratum corneum, and the transport of OE from the stratum corneum to the active epidermis does not become the speed limit factor. The barrier properties of the stratum corneum are derived only partially from the stratum corneum lipids, whereas the resistance produced by the stratum corneum cell membrane is an important component of the stratum corneum barrier properties. At the same time, the stratum corneum lipids may also be the way of OE diffusion. These substances affect the distribution of the latter in the stratum corneum by solubilizing lipophilic drugs. The promoting effect of the accelerator 1,8-eucalyptol (1,8-CN) on OE also depends in part on the presence of stratum corneum lipids, altering the permeability of the lipid pathway through a reversible physical interaction .