活血止痛纳米凝胶贴膏经皮渗透特性及药效评价  

Evaluation on Transdermal Absorption Properties and Efficacy of Huoxue Zhitong Cataplasm

作　　者：姚瑶[1,2] 冯伟红[2] 王岚[2] 易红[2] 梁日欣[2] 何爱萍[3] 殷晓杰[2] 杜茂波[2] 刘淑芝[2] 

机构地区：[1]首都医科大学,北京100069 [2]中国中医科学院中药研究所,北京100700 [3]江西中医药大学,江西南昌330004

出　　处：《中国中医药信息杂志》2017年第2期70-75,共6页Chinese Journal of Information on Traditional Chinese Medicine

基　　金：国家科技重大专项-重大新药创制(2014ZX09301306009)

摘　　要：目的研究微乳/醇质体对活血止痛凝胶贴膏的经皮渗透特性及对药效的影响。方法采用改进的Franz扩散池法进行体外透皮试验,以离体小鼠皮肤为透过屏障,采用超高效液相色谱法测定指标成分丹皮酚、丁香酚、水杨酸甲酯的含量,评价活血止痛凝胶贴膏的经皮渗透效果。并采用小鼠醋酸扭体实验比较其抗炎镇痛作用。结果凝胶贴膏、微乳凝胶贴膏和醇质体凝胶贴膏丹皮酚24 h累计透过率分别为65.30%、61.30%、60.20%,丁香酚24 h累计透过率分别为51.08%、54.71%、55.66%,水杨酸甲酯24 h累计透过率分别为49.20%、65.17%、72.15%。微乳凝胶贴膏大剂量组、醇质体凝胶贴膏中剂量组对减少模型动物腹腔内毛细血管的炎性渗出、降低毛细血管通透性有较好的作用(P<0.05)。结论基于微乳/醇质体技术的复合型纳米载体可使活血止痛凝胶贴膏中有效成分透过皮肤屏障的能力更优,从而提高药效。Objective To study the effects of microemulsion/ethosomes on transdermal absorption properties and efficacy of Huoxue Zhitong Cataplasm. Methods The improved Franz diffusion cells were used for the in-vitro permeation experiment with rat skins as the barriers, which was used to evaluate the transdermal absorption properties. In the erxeriment, the contents of paeonol, eugenol and methyl salicylate were used as markers, and detected by ultra performance liquid chromatography to evaluate the transdermal absorption effects. The anti-inflammatory and analgesia activity were evaluated through the writhing plate experiments. Results The cumulative release rate of paeonol in Huoxue Zhitong Cataplasm, Microemulsion Huoxue Zhitong Cataplasm and Ethosomes Huoxue Zhitong Cataplasm were, in order, 65.30%, 61.30% and 60.20% in 24 h; eugenol were, in order, 51.08%, 54.71% and 55.66% in 24 h; methyl salicylate were, in order, 49.20%, 65.17% and 72.15% in 24 h. Furthermore, Microemulsion Huoxue Zhitong Cataplasm high-dose group and Ethosomes Huoxue Zhitong Cataplasm medium-dose group had good effects on reducing the inflammatory exudate of peritoneal capillary and capillary permeability（P0.05） in animal models. Conclusion Huoxue Zhitong Cataplasm based on microemulsion/ ethosomesnano-technology has good transdermal absorption properties and efficacy.

关 键 词：活血止痛凝胶贴膏 微乳 醇质体 透皮试验 抗炎 镇痛 

分 类 号：R283.5[医药卫生—中药学]