促渗剂对后交联祖师麻凝胶贴膏体外经皮渗透影响的研究

Effect of Penetration Enhancers on Transdermal Penetration of Post-crosslinking Daphnes Giraldii Cortex Gel Plaster In Vitro

关键词:  祖师麻  后交联凝胶贴膏  经皮渗透  促渗剂  祖师麻甲素

Key words:  Daphnes Giraldii Cortex  post-crosslinking gel plaster  transdermal absorption  penetration enhancer  daphnetin

摘要:

目的 考察不同促渗剂对后交联祖师麻凝胶贴膏中药效成分祖师麻甲素体外经皮渗透特性的影响,筛选出其最佳的透皮促渗剂。方法 采用Franz扩散池法,以离体小鼠皮肤和Strat-M™膜为渗透屏障进行体外透皮试验,采用单因素及正交试验法,以祖师麻甲素72 h内单位面积的累积透过量为评价指标,考察冰片、薄荷脑、樟脑对祖师麻甲素的促渗效果。结果 以离体小鼠皮肤和Strat-M™人工膜为透皮屏障时,祖师麻甲素72 h内单位面积的累积透过量分别为33.85,15.96 μg·cm^-2,稳态透皮速率分别为4.451 2,2.394 5 μg·cm^-2·h^-1,增渗倍数分别可达4.255 0,1.746 4。结论 后交联祖师麻凝胶贴膏以1%薄荷脑、1%冰片、2%樟脑联用时促渗效果最佳。

Abstract:

OBJECTIVE To investigate the effect of different penetration enhancers on the external transdermal absorption characteristics of the pharmacodynamic components of daphnetin in post-crosslinking Daphnes Giraldii Cortex gel plaster and screen out the best penetration enhancers. METHODS In vitro transdermal test was carried out with mouse skin and Strat-M™ membrane as the penetration barrier by Franz diffusion cell method. Using the cumulative penetration rate per unit area of daphnetin within 72 h as the evaluation index, by single factor experiment and orthogonal experiment to investigate the promoting effect of borneol, menthol and camphor on the daphnetin. RESULTS When in vitro mouse skin and Strat-M™ membrane were used as transdermal barrier, the cumulative transdermal flux per unit area was 33.85, 15.96 μg·cm^-2 for 72 h, and the steady transdermal rate was 4.451 2, 2.394 5 μg·cm^-2·h^-1. The infiltration multiple was 4.255 0 and 1.746 4. CONCLUSION The best penetration enhancer of post-crosslinking Daphnes Giraldii Cortex gel plaster is 1% menthol, 1% borneol and 2% camphor.