川芎挥发油对氟比洛芬渗透离体大鼠皮肤的促进作用

目的：研究川芎挥发油的体外促透作用及机制。方法：超临界萃取川芎挥发油，气相色谱-质谱法分析成分，以大鼠皮肤为渗透屏障，氟比洛济为模型药物，Franz扩散池法考察透皮特性，HPLC法测定大鼠皮肤中药物含量。结果：苯酞（91．15％）和萜烯（5．19％）组成的川芎挥发油具有显著的促透作用，但其强度低于同浓度的油酸;3％的挥发油具有最强的促透作用，随着挥发油浓度的增加，促透作用反而下降；透皮流量和皮肤滞留药量之间具有相关性。结论：川芎挥发油能显著增强氟比洛芬的透皮吸收，其作用机制可能是通过破坏角质层的结构，增加皮肤中的药物分配。其促透的物质基础可能是苯酞化合物。

Enhancing effect of essential oils from Ligusticum chuanxiong Hort. on the permeation of flurbiprofen through isolated rat skin

Objective: To evaluate the enhancing effect of essential oils from Ligusticum chuan-xiong Hort. (chuanxiong oil) on skin permeation in vitro of flurbiprofen and its mechanism. Methods:Chuanxiong oil was extracted by supercritical fluid carbon dioxide and its major constituents were identified by gas chromatography-mass spectrometry analysis. Rat skin was used as permeation barrier and flurbiprofen in rat skin was selected as a model drug. The transdermal characteristics were investigated using Franz diffusion cell. The content of flurbiprofen was measured by HPLC method. Results:Chuanxiong oil, composed of phthalides (91. 15%) and terpenes (5. 19%) .showed a marked permeation enhancing effect,but the enhancement was lower than that of oleic acid at the same concentration. The gel containing 3% chuanxiong essential oil exhibited the greatest permeation enhancing effect. The permeation enhancement was reduced with increasing the oil concentration. There was a correlation between transdermal flux and drug accumulation in the skin. Conclusion;Chuanxiong oil enhances significantly percutaneous absorption of flurbiprofen. The possible mechanism of the action is the disruption of the structure of stratum corneum and the increment of flurbiprofen distribution into stratum corneum. The chemical base of skin permeation enhancing effect is possibly phthalides.