中国中药杂志

2013, v.38(16) 2623-2627

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苦参地龙纳米乳凝胶的制备及其离体透皮吸收研究
Preparation of Kushen-Dilong nanoemulsion gel and transdermal characterization in vitro

贺葵邦;王英姿;冯艾灵;段飞鹏;李彩霞;孙秀玉;
HE Kui-bang,WANG Ying-zi*,FENG Ai-ling,DUAN Fei-peng,LI Cai-xia,SUN Xiu-yu (School of Chinese Pharmacy,Beijing University of Chinese Medicine,Beijing 100102,China)

摘要(Abstract):

目的:制备苦参地龙纳米乳和纳米乳凝胶剂,并对其含量、理化性质和体外透皮特性进行考察。方法:将苦参总碱溶入油相IPM,加入表面活性剂EL35、助表面活性剂无水乙醇溶解混合为含药内相,恒温搅拌至均匀;将地龙提取物溶于去离子水中,在室温下边搅拌边缓慢滴加到含药内相中,恒速搅拌至澄清透明,得苦参地龙纳米乳。采用HPLC测定纳米乳中苦参碱和氧化苦参碱的含量;采用透射电镜和激光粒径测定仪分别考察纳米乳的形态和粒径。以NP700为基质,制备苦参地龙纳米乳凝胶,并采用Franz扩散池对纳米乳、纳米乳凝胶的体外透皮特性进行考察。结果:制备的苦参地龙纳米乳为O/W型微乳,外观圆整、均匀,粒径20.6 nm,含量稳定。苦参地龙纳米乳、苦参地龙纳米乳凝胶、苦参地龙水溶液、苦参地龙水凝胶的稳态渗透速率分别为0.148 4,0.118 3,0.030 6,0.032 1 mg·cm-2·h-1。结论:苦参地龙纳米乳、纳米乳凝胶的24 h累积渗透量和渗透速率均优于水溶液、水凝胶,可为苦参地龙药对经皮给药提供一种新的剂型。
Objective: To prepare Kushen-Dilong nanoemulsion and nanoemuls-ion gel,and investigate its content,physical and chemical properties.Their transdermal properties in vitro were studied as well.Method: IPM acted as oil phase,EL35 as surfactant,EtOH as cosurfactant,Pheretima aqueous solution was added dropwise to the oil phase to prepare Kushen-Dilong nanoemulsion at room temperature using magnetic stirring.HPLC was used to determine the content of matrine and oxymatrine in the nanoemulsion.Transmission electron microscopy and laser particle size analyzer was used to determine the shape and size of the nanoemulsion.NP700 was used as substrate to prepare Kushen-Dilong nanoemulsion gel.Franz diffusion cell was used for the nanoemulsion and gel transdermal characteristics in vitro.Result: The Kushen-Dilong nanoemulsion was O/W nanoemulsion,its uniform particle size was 20.6 nm with roundness appearance and stable content.The steady-state permeation rate of Kushen-Dilong nanoemulsion,nanoemulsion gel,saturated aqueous solution,hydro gel were 0.148 4,0.118 3,0.030 6,0.032 1 mg·cm-2·h-1,respectively.Conclusion: The 24 h cumulative infiltration and infiltration rate of Kushen-Dilong nanoemulsion and nanoemulsion gel were better than the saturated aqueous solution and hydro gel,which could provide a new dosage form for Kushen-Dilong transdermal drug delivery.

关键词(KeyWords): 苦参;地龙;纳米乳凝胶;制备;透皮吸收
Sophora flavescens;Pheretima;nanoemulsion gel;transdermal absorption

Abstract:

Keywords:

基金项目(Foundation): 中药制药过程新技术国家重点实验室开放基金项目(SKL2010M0302);; 北京中医药大学复方中药制药研究创新团队项目(2011-CXTD-13);; 北京中医药大学自主选题项目(2011-JYBZZ-JS048);;

作者(Author): 贺葵邦;王英姿;冯艾灵;段飞鹏;李彩霞;孙秀玉;
HE Kui-bang,WANG Ying-zi*,FENG Ai-ling,DUAN Fei-peng,LI Cai-xia,SUN Xiu-yu (School of Chinese Pharmacy,Beijing University of Chinese Medicine,Beijing 100102,China)

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