祖师麻总香豆素体外透皮特性考察

Investigation of in vitro Transdermal Permeability of Total Coumarins in Daphne giraldii

摘要:

目的: 考察祖师麻总香豆素有效部位的透皮吸收特性及促渗剂对其透皮行为的影响。方法: 采用V-C水平扩散池法,以祖师麻甲素的平均渗透系数、累积渗透量和皮肤蓄积量为指标,考察祖师麻总香豆素的透皮吸收动力学特性,并考察不同促渗剂对其促透作用的影响。采用HPLC测定祖师麻甲素含量,色谱条件为Kromasil C₁₈色谱柱(4.6 mm×250 mm,5 μm),流动相乙腈-0.1%磷酸水(22:78),检测波长327 nm,进样量20 μL,流速1.0 mL·min^-1。结果: 祖师麻甲素透皮吸收质量浓度与时间均表现为一级动力学模式。1%,3%,5%冰片的吸收时滞分别为2.3,2.9,3.3 h。氮酮、丙二醇、冰片及氮酮与丙二醇合用等促渗剂均能明显促进祖师麻甲素的透皮吸收,总体促渗效果为氮酮>冰片>氮酮与丙二醇合用>丙二醇>无促渗剂。结论: 选用3%氮酮作为祖师麻总香豆素有效部位的促渗剂。

Abstract:

Objective: To investigate transdermal absorption characteristics of total coumarins in Daphne giraldii and influence of penetration enhancers on transdermal behavior of these ingredients. Method: Valia-Chien diffusion cell was adopted,with the average permeability coefficient,cumulative permeation amounts and skin accumulation amounts of daphnetin as indexes,transdermal absorption kinetics characteristics and effects of penetration enhancer on it were investigated.The content of daphnetin was determined by HPLC,chromatographic conditional were as follows:Kromasil C₁₈ column(4.6 mm×250 mm,5 μm),mobile phase of acetonitrile-0.1% phosphoric acid(22:78),detection wavelength 327 nm,injection volume 20 μL,flow rate 1.0 mL·min^-1. Result: Transdermal concentration of daphnetin and time showed a kinetic mode.Absorption time-lag of 1%borneol,3%borneol,5%borneol were 2.3,2.9,3.3 h,respectively.Azone,1,2-propanediol and borneol could obviously promote transdermal absorption of daphnetin,order of the overall penetration effect was azone>borneol>azone and 1,2-propanediol>1,2-propanediol>no penetration enhancer. Conclusion: 3% Azone was the best penetration enhancer for total coumarins in D. giraldii.