口疳散穴位贴敷的制备工艺及体外透皮吸收研究

Research of Preparation and in vitro Percutaneous Absorption of Kougan San Acupoint Application

目的:考察不同制备工艺,包括药材粉碎方法、黏合剂以及透皮吸收剂对穴位贴敷有效成分透皮吸收的影响。方法:以裸鼠腹部皮肤为体外透皮实验材料,以吴茱萸碱为指标成分,用改良Franz扩散池法建立透皮吸收试验方法,收集穴位贴敷的透皮接受液,用高效液相色谱法测定其吴茱萸碱的含量,计算其累积透皮量、透皮速率和皮肤滞留量。结果:吴茱萸碱可以透过离体皮肤,药材粉末使用超微粉能显著提升吴茱萸碱的累积透皮量(P<0.01)。醋为黏合剂相较于水,其累积透皮量显著增加(P<0.001);再加入3%氮酮能显著增加吴茱萸碱的累积透皮量(P<0.05)。结论:药材粉末为超微粉,用醋作为黏合剂并加入3%氮酮,所制得的口疳散穴位贴敷透皮吸收效果最佳。

Objective:To investigate the effects of different preparation techniques,such as crushing methods an use of adhesives and transdermal absorbents,on transdermal absorption of active ingredients in the Kougan San Acupoint Application(KSAA).Methods:Skins of nude mice were used for transdermal absorption tests with a modified Franz diffusion pool method,percutaneous fluids of KSAA were collected.The contents of evodiamine in the percutaneous fluids were determined by high performance liquid chromatography,and the cumulative transdermal volume,transdermal rate and skin retention of evodiamine were calculated.Results:The evodiamine penetrated through the skin in vitro.The cumulative transdermal volume of evodiamine was significantly increased by using ultrafine powder crushing(P<0.01).The cumulative transdermal volume was significantly higher with vinegar than with water as an adhesive(P<0.001).The cumulative transdermal volume of evodiamine was significantly increased by the addition of 3%azone.Conclusions:The optimal transdermal absorption of KSAA may achieved by using vinegar as adhesive,being crushed to ultrafine powder and adding 3%azone.