Hashida M, Mukai E, Kimura T, Sezaki H
J Pharm Pharmacol. 1985 Aug;37(8):542-4. doi: 10.1111/j.2042-7158.1985.tb03063.x.
The percutaneous permeation characteristics of two lipophilic mitomycin C derivatives with aromatic moieties were determined using excised hairless mouse and rat skins and compared with those of mitomycin C (MMC). 1a-N-Benzylmitomycin C penetrated more readily through both kinds of skin than MMC without metabolic conversion. 1a-N-Benzyloxycarbonylmitomycin C effected a 4-fold increase in the delivery of MMC through the rat skin and was completely converted to MMC by an enzyme in rat skin. However, saturation of the metabolic conversion activity was observed in the hairless mouse skin.
使用切除的无毛小鼠和大鼠皮肤测定了两种带有芳香基团的亲脂性丝裂霉素C衍生物的经皮渗透特性,并与丝裂霉素C(MMC)的经皮渗透特性进行了比较。1a-N-苄基丝裂霉素C比MMC更容易穿透这两种皮肤,且无代谢转化。1a-N-苄氧羰基丝裂霉素C使MMC通过大鼠皮肤的递送量增加了4倍,并被大鼠皮肤中的一种酶完全转化为MMC。然而,在无毛小鼠皮肤中观察到代谢转化活性的饱和。