白芷香豆素类有效部位体外透皮特性研究

Study on the transdermal permeability of coumarins in Radix Angelica Dahurica in vitro

目的 考察白芷香豆素类有效部位的透皮吸收特性及促透剂对其透皮行为的影响。方法 以有效成分欧前胡素为定量考察指标 ,通过V C水平扩散池用HPLC测定指标成分的透皮吸收动力学特性及促进剂的促透作用。结果 以欧前胡素为指标经离体小鼠、家兔、大鼠和人体皮肤的渗透系数分别为 2 4 .1,2 2 .9,11.5和 8.9,而月桂氮酮 (Azone)、冰片、油酸有明显的促透作用 ,其中 2 %月桂氮酮和冰片使渗透系数分别增加了 4 .9和 6 .2倍。结论 白芷香豆素类有效部位在大鼠皮肤中渗透系数与人体皮肤接近 。

OBJECTIVE: To investigate the characteristics of transdermal absorption of coumarins as the effective components in Radix Angelica Dahurica and the influence of penetration enhancers on the transdermal action of the drug. METHODS: The dynamic profiles and the permeability coefficients of imperatorin through different skins were investigated in Valia-Chien diffusion cell and determined by HPLC. The effects of alcohol, azone, oleic acid and borneol as penetration enhancers on the transdermal permeability of the effective part were also analyzed. RESULTS: The permeability coefficients of the imperatorin for the mouse, rabbit, rat and human skins were 24.1,22.9,11.5 and 8.9 respectively. Azone, borneol and oleic acid had promotions actions on percutaneous absorption of imperatorin. In addition, the permeability coefficients of imperatorin in 2% azone and borneol were 4.9 and 6.2 times as much as that in normal saline. CONCLUSION: The transdermal characteristics of the coumarins through rat skin was close to that of human skin. Azone and borneol as penetration enhancers may promote the permeability of the coumarins through the skin.