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角质层(stratumcorneum,SC)是皮肤给药的主要屏障,无论是局部经皮的皮内给药还是经皮吸收进入体循环发挥全身作用都必须克服SC的屏障作用。但绝大部分药物都难以有效地透过SC,在众多克服SC的方法中,化学渗透促进剂(chemical penetration enhancers,CPE)的应用最广泛。除传统的醇类、亚砜类、脂肪酸类、酯类、氮酮、多元醇类等,又发现或合成了许多新型高效的促进剂。文中对近年来国内外关于新型渗透促进剂的文献进行综述,以期为合成和发现更加安全、高效的渗透促进剂提供线索。
Stratum corneum (SC) is the main barrier for dermal administration and the barrier function of SC must be overcome either by topical transcutaneous intradermal administration or percutaneous absorption into systemic circulation for systemic effects. However, it is difficult for most drugs to penetrate SC effectively. Among the many ways to overcome SC, chemical penetration enhancers (CPEs) are the most widely used. In addition to the traditional alcohols, sulfoxides, fatty acids, esters, azone, polyols, etc., have also discovered or synthesized many new and highly effective accelerators. In this paper, the literature review on new penetration enhancers at home and abroad in recent years is reviewed in order to provide clues for the synthesis and discovery of safer and more efficient penetration enhancers.