逐淤止痛远红外灸贴中芍药苷、阿魏酸及藁本内酯的透皮特性研究  

Study on transdermal properties of paeoniflorin, ferulic acid and ligustilide in Zhuyu Zhitong far-infrared moxibustion plaster

作　　者：毕建云[1] 杨东 杨文翠 BI Jianyun;YANG Dong;YANG Wencui(Experimental Center of Shandong University of Traditional Chinese Medicine,Jinan,Shandong,250355 P.R.China;Yidu Central Hospital of Qingzhou,Weifang,Shandong,262500 P.R.China)

机构地区：[1]山东中医药大学,山东济南2503553 [2]青州市益都中心医院,山东潍坊262500

出　　处：《华西药学杂志》2022年第5期493-497,共5页West China Journal of Pharmaceutical Sciences

基　　金：2022年山东省卫生健康政策研究重点课题(WZY202296);山东中医药大学2021年度创新创业教育教学研究课题(CXCY202115);山东中医药大学中药学专业认证专项教学改革团队项目(2021)。

摘　　要：目的 研究逐淤止痛远红外灸贴中芍药苷、藁本内酯及阿魏酸的体内外透皮性能。方法 根据《中国药典》规定的释放度测定法测定体外释放度;采用Franze扩散池法测定药物的体外透皮性能;通过小鼠在体透皮实验、药动学实验及皮肤组织HE染色考察药物的在体透皮性能。结果 凝胶贴组与凝胶贴辅助艾灸组中芍药苷、藁本内酯、阿魏酸的体外释放及体外透皮均符合Higuchi方程;体外透皮实验中凝胶贴辅助艾灸组中3种成分的累积透过量与累积皮下滞留量较凝胶贴组均相应增加;在体透皮实验与体外透皮实验的结果相似,阿魏酸的结果略有不同;HE染色发现:使用凝胶贴和凝胶贴辅助艾灸后,皮肤结构无损伤,角质层组织变薄,棘层细胞、基底层细胞排列松散,整体的皮肤结构趋于变薄。结论 凝胶贴中3种成分的透皮性能为藁本内酯>阿魏酸>芍药苷;该制剂属于皮肤限速型经皮给药制剂,其透皮机制主要是通过破坏皮肤角质层微观结构和通过皮肤附属器,使药物经皮渗透从而发挥治疗作用。OBJECTIVE To study the skin permeability of paeoniflorin, ligustilide and ferulic acid in Zhuyu Zhitong far-infrared moxibustion plaster.METHODS In vitro release rate was determined by release rate assay;in vitro transdermal properties of the drug were determined by Franze diffusion cell assay;and in vivo transdermal properties of the drug were investigated by mice in vivo transdermal experiment, pharmacokinetics experiment and HE staining of skin tissues.RESULTS The release rates of paeoniflorin, ligusticide and ferulic acid in the gel group and the gel plaster assisted group accords with those in the Higuchi equation.The cumulative penetration and cumulative subcutaneous retention of the three components in the adhesive assistant moxibustion group increased correspondingly compared with those in the gel group.In vivo transdermal test was similar to those in vitro skin penetration test, and ferulic acid was slightly different;HE staining revealed the skin structure was basically complete, the keratosis was thinner, the keratin fragments were increasing, the spinous layer cell gap was increasing, and the basal layer cells loosely arranged.CONCLUSION The transdermal properties of the three components in gel paste are ligusticide > ferulic acid > paeoniflorin.The preparation is a dermal speed limiting transdermal drug delivery system, and its transdermal mechanism is mainly through the destruction of the skin cuticle microstructure and the use of skin appendages to make the drug play a therapeutic role through the skin.

关 键 词：逐淤止痛远红外灸贴 芍药苷 藁本内酯 阿魏酸 体内透皮 体外透皮 透皮特性 

分 类 号：R94[医药卫生—药剂学] R96[医药卫生—药学]