摘要
研究了桉叶素促进５－氟尿嘧啶渗透通过离体大鼠皮肤的作用，其增加药物渗透系数约达９３倍。桉叶素提高了分配系数，但对扩散系数的增加更大。去除角质层，药物的渗透障碍完全消失。与全皮相比，角质层去除后药物的渗透系数增加１６６倍，表明影响极性药物渗透的主要障碍是角质层。促渗效果可能是扩散和分配综合作用的结果，其中扩散是主要作用。
Cineole (1,8 cineole, eucalyptol) was evaluated as a penetration enhancer towards 5 fluorouracil (5 FU) using excised rat skin. It caused a near 93 fold increase in drug permeability coefficient. The enhancer gives increased partition coefficient but the diffusion coefficient values were higher. Removal of the stratum corneum has eliminated the resistance to the drug permeation. After removal of the stratum corneum the permeability coefficients of 5 FU increased by a factor of 166 compared with full thickness skin with the stratum corneum intact, showing that main resistance to the permeation of polar drug lies in the stratum corneum. The mode of action of the accelerant may be described by combined process of partition and diffusion, the diffusion process being dominant.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1999年第2期86-89,共4页
Journal of China Pharmaceutical University
