Sugibayashi K, Hosoya K, Morimoto Y, Higuchi W I
J Pharm Pharmacol. 1985 Aug;37(8):578-80. doi: 10.1111/j.2042-7158.1985.tb03073.x.
The effect of the percutaneous absorption enhancer, Azone, on the transport of 5-fluorouracil across hairless rat skin has been investigated by an in-vitro permeation technique using 2-chamber diffusion cells. Azone (3% w/v) emulsions were used. Azone enhanced the permeability of drug 10-100 times across the full-thickness skin although there was a lag time about 10 h. The long lag time, however, disappeared with Azone pretreatment. Azone also affected the transport across stripped skin. These results suggest that Azone mainly affects the stratum corneum. It seems to change the diffusivity of drug in that layer and is not so effective against diffusivities in the epidermis and dermis.
采用双室扩散池体外渗透技术,研究了经皮吸收促进剂氮酮对5-氟尿嘧啶透过无毛大鼠皮肤的影响。使用了3%(w/v)的氮酮乳剂。尽管存在约10小时的滞后时间,但氮酮使药物透过全层皮肤的渗透率提高了10至100倍。然而,氮酮预处理后,较长的滞后时间消失了。氮酮也影响药物透过去角质皮肤的转运。这些结果表明,氮酮主要影响角质层。它似乎改变了药物在该层中的扩散系数,而对药物在表皮和真皮中的扩散系数影响不大。