不同浓度氮酮、薄荷醇对盐酸特比萘芬体外经皮渗透作用的影响

Effect of the Various Concentration of Azone and Menthol on the in vitro Percutaneous Penetration of Terbinafine through Excised Canine Epidermis

为选择促进盐酸特比萘芬(TBF)透皮扩散作用的促渗剂,选用立式Franz扩散池,以犬离体皮肤为透皮屏障,通过计算含不同浓度氮酮(AZ)、薄荷醇(MT)组盐酸特比萘芬透皮试验的累积渗透量Q、稳态流速Jss、渗透系数KP和增渗比ER等参数来比较促渗效果。结果显示试验中所有组别促渗剂都具有促渗作用,作用由强至弱依次为1%AZ**>5%MT**>3%AZ**>3%MT**>1%MT*>5%AZ*,其中薄荷醇组促渗效果与浓度呈线性正相关,而氮酮组则呈线性负相关。虽然各组促渗剂均起促进作用,但薄荷醇组的效果优于氮酮组,加之薄荷醇属天然物质,毒副作用低,所以更适合作为药物外用制剂的促渗剂。

This experiment was conducted to study permeation-enhancing effect of various concentration of Azone and menthol on the in vitro percutaneous penetration of terbinafine （TBF） through canine epidermis. Modified Franz vertical glass diffusion cells were used and excised canine epidermis was chose as transdermal barrier. The in vitro permeation effects of every combination of TBF with various concentration enhancers were evaluated through calculating and comparing the cumulative penetration amount, steady-state flux, permeability coefficient and enhancement ratio. The results revealed that various concentration of enhancers had the permeationenhancing effect, the sequence of effect was 1% AZ^＊＊ 〉 5 % MT^＊＊ 〉 3 % AZ^＊＊ 〉 3 % MT^＊＊ 〉 1%MT^＊ 〉5%AZ^＊. The linear correlation between the effect of combinations of TBF with menthol and the concentration of menthol was positive, while the linear correlation between the effect of combinations of TBF with Azone and the concentration of Azone was negative. Though all combinations of TBF with enhancers had the enhancement effect, the effect of menthol was better than that of Azone. Besides, the menthol is a natural product with low toxicity and side effect, so it is a preferable enhancer for the external preparation.