大蒜辣素软膏的体外透皮吸收特性研究

Study on transdermal absorption characteristics of allicin ointment in vitro

目的研究大蒜辣素软膏在离体大鼠皮肤的吸收特性。方法通过Franz扩散池,建立离体大鼠完整背部皮肤及去角质层皮肤的透皮模型,采用超高效液相色谱-质谱-质谱串联法(UPLC-MS-MS)测定大蒜辣素软膏透皮吸收液中大蒜辣素的含量,测定大蒜辣素软膏的体外透皮吸收特性,并评价该大蒜辣素累积透过量及渗透速率。结果大蒜辣素5 h内体外经皮渗透量Q与时间t线性关系较好,均符合Higuchi动力学过程,回归相关系数(r)均达到0.99以上。完整皮肤的透皮速率J为12.306μg·cm^(-2)·h^(-1),去角质层皮肤的J为58.353μg·cm^(-2)·h^(-1),去角质层皮肤的J高于完整皮肤。结论大蒜辣素软膏有效成分可经皮渗透,主要以原型形式吸收,角质层厚度是影响大蒜辣素软膏透过皮肤的重要因素。

Objective To study the absorption characteristics of allicin ointment on isolated rat skin.Methods A transdermal model of intact dorsal skin and exfoliated skin of the rats was established using a Franz diffusion cell.The indicator content of allicin in the transdermal absorption solution of allicin ointment was determined using ultra-high performance liquid chromatography mass spectrometry tandem mass spectrometry(UPLC-MS-MS).The in vitro transdermal absorption characteristics of allicin ointment were determined,and the cumulative transmittance and permeation rate of allicin was evaluated.Results The linear relationship between the in vitro transdermal penetration of allicin Q within 5 hours and time t was good,which conformed to Higuchi kinetic process.The regression correlation coefficients(r)were all above 0.99.And the transdermal rate of intact skin J was 12.306μg·cm^(-2)·h^(-1),J of exfoliated skin was 58.353μg·cm^(-2)·h^(-1),the J of exfoliated skin was much higher than that of intact skin.Conclusion The effective ingredients of allicin ointment can penetrate through the skin and are mainly absorbed in the prototype form.