盐酸布替萘芬乳膏的离体透皮吸收研究

目的:研究盐酸布替萘芬乳膏对离体豚鼠皮的透皮吸收情况,并对自制乳膏与国内外已上市产品的离体透皮渗透量进行比较。方法:采用透皮吸收仪,皮片涂药后不同时间采样,用高效液相色谱法测定样品中盐酸布替萘芬的浓度。结果:在50%乙醇生理盐水释放液中,国外产品、国内产品和自制产品36 h透皮渗透量分别只有0.061 89,4.661,和0.289 7μg.cm-2,盐酸布替萘芬乳膏透皮渗透量很低,三者无显著性差异。结论:自制盐酸布替萘芬乳膏的豚鼠离体透皮吸收程度与国外同类品种相当。盐酸布替萘芬乳膏主成分大部分滞留在皮肤,只有极少数透过皮肤屏障,有利于其发挥局部治疗作用。

In vitro percutaneous absorption of butenafine hydrochloride cream

Objective: To investigate the percutaneous absorption of butenafine hydrochloride cream through guinea pig skins,and compare in vitro penetration release of self-made cream with domestic and overseas listed products.Methods: Using the percutaneous absorption instrument,samples were collected at various time points after the drug was applied.The concentrations of butenafine hydrochloride in the samples were measured by HPLC.Results: The 36 h penetration releases of butenafine hydrochloride across guinea pig skins in 50% ethanol-saline solution of foreign products,domestic products and self-made products were only 0.061 89,4.661 and 0.289 7 mg·cm-2,respectively.The percutaneous absorption of butenafine hydrochloride cream was very low,and there was no significant difference among three products.Conclusion: The penetration absorbency through guinea pig skins of self-made cream is similar to foreign products.Majority of the main components of butenafine hydrochloride cream remains on the surface of the skins,only a few crosses through the skin barrier,so it is suitable to local application.