薄荷醇对两种不同性质化合物体外经兔皮吸收的影响

目的 :以吲哚美辛(Ind)和双氯芬酸钠(Dcs)为模型药物 ,研究薄荷醇对两种不同性质化合物的促透特性 ,并探讨其与氮酮联用时的促透效果。方法:在离体透皮实验装置上进行透皮吸收试验和贮库效应的研究。结果 :薄荷醇对两种化合物的体外透皮吸收均有明显的促进作用 ,时滞明显缩短 ;单独或与氮酮联用时 ,Ind的增渗倍数强于Dcs ;联用比单独应用薄荷醇促透效果更明显 ,时滞均显著延长 ,尤其是Dcs延长作用更明显。贮库效应的研究发现 ,薄荷醇组对Ind的透皮速率比空白对照组明显增加 (P<0 05) ,时滞显著延长(P<0 01) ;联用比单用薄荷醇促透效果更明显 ,但Dcs组的透皮速率比空白对照组显著减少 (P<0 01) ,时滞比薄荷醇组显著缩短。结论 :薄荷醇对脂溶性化合物的体外透皮吸收促进作用强于水溶性化合物 ,并具有明显的贮库效应 ;联用氮酮对脂溶性化合物的促透作用更明显

Effect of L－ menthol on Two Compounds With Different Characteristics in Percutaneously Penetrating Isolated RabbitSkin

OBJECTIVE:Indomethacinum(Ind) and diclofenac sodium(Dcs) were taken as model drugs to study the enhancing effect of l-menthol on percutaneous absorption of two compounds with different characteristics,and to probe into the effect of combined use of l-menthol with azone.METHODS:Percutaneous penetration experiment was performed on in vitro device and deposit effect was observed with vivoperception.RESULTS:l-menthol could significantly enhance the percutaneous absorption and shorten the lag times(T1ag) of both Ind and Dcs.The enhancing effects of l-menthol,used either alone or in combination with azone,were several times stronger on Ind than on Dcs.Combined use of two enhances was more effective in enhancing penetration and longer in T1ag than single use of l-menthol,especially for Dcs.The study on deposit effect showed that l-menthol could increase the penetration rate than control agent(P<0.05) and prolong the Tlag(P<0.01).Combined use of both enhances was more effective in penetration than single use of l-menthol but markedly decreased the penetration rate of Dcs in comparison with control agent(P<0.01) and obviously shorten the Tlag compared with single l-menthol.CONCLUSION:l-menthol has stronger enhancing effect on fat soluble compound than on water soluble compound and shows marked deposit effect.Combined use of l-menthol with azone can further increase the enhancing effect on fat soluble compound.