3种吸收促进剂对酮基布洛芬经不同皮肤层渗透的影响

目的：对不同性质的吸收促进剂影响药物经不同皮肤层渗透的差异进行评价。方法：选择氮酮（AZ），肉豆蔻酸异丙酯（IPM）和单月桂酸甘油酯（GML）为透皮促进剂，以酮基布洛芬为模型药物，采用Franz吸收池法，考察药物单儿或与促进剂合用时，完整皮肤和剥离角质层皮肤的透皮能力。结果：剥离角质层皮肤可明显增加酮基布洛芬的透皮层。3种吸收促进剂对药物经完整皮肤的促透能力为IPM＞GML＞AZ，对药物经剥离角质层皮肤的促透能力为GML＞IPM＞AZ。结论：皮肤的条件能明显影响酮基布洛芬的经皮渗透；吸收促进剂对酮基布洛芬经不同皮肤层的促透能力有差异。

INFLUENCE OF 3 KINDS OF ENHANCERS ON THE PERMEABILITY OF KETOPROFEN VIA INTACT OR STRIPPED SKIN

OBJECTIVE To evaluate the permeability of the drug with or without the enhancers through intact or stripped skin.METHODS Ketoprofen was chosen as a model drug. Its patches with or without azone (AZ), isopropyl myristate (IPM), or glycerol monolaurate (GML) were prepared. The in vitro transdermal permeation experiment via different rat skin layers was carried out. RESULTS The permeability of ketoprofen was significantly increased via stratum corneum-stripped skin, compared with that via intact skin. The 3 kinds of enhancers selected could also increase the permeability of the drug, which was IPM > GML or AZ in order of the case via intact skin. However, the order of increasing action was GML > IPM > AZ for the case via stripped skin. CONCLUSION The skin condition exerts some effects on drug permeability. The enhancers have different contribution to the drug permeability through stratum layer or viable skin layer. These data and methods also represent a novel approach to evaluate the effects of skin damage and skin disease on drug percutaneous absorption.