【作者】 孙丽梅；

【导师】 周忠光；

【作者基本信息】 黑龙江中医药大学 ， 中西医结合基础， 2011， 博士

【摘要】 [目的]为了阐明脐中穴给药的科学性和理论依据,建立脐中穴经皮给药的共性技术和质量评价体系,为创建脐中穴经皮给药的现代制剂提供科学依据。[方法]查阅了脐中穴经皮给药文献资料,从经络学、解剖学、生理学、临床应用、制剂学、药物透皮吸收理论等方面进行研究,分别以白芍和延胡索药材的乙醇提取物为原料药,利用现代新型的赋形剂不饱和脂肪酸甘油脂、可可脂、聚乙二醇、甘油-明胶-水、泊洛沙姆等为基质,以脂溶性氮酮、水溶性氮酮及二甲基亚砜为透皮吸收促进剂制备成贴膏剂,通过Franz扩散池模拟人体透皮吸收过程,进行了的不同给药系统的工艺制备研究；对豚鼠进行了皮肤刺激性、致敏实验,通过小鼠扭体法和热板法进行药效学研究。[结果]延芍贴膏剂以甘油-明胶-水为基质,以3%脂溶性氮酮为促渗剂时透皮效果最佳；延芍栓片对豚鼠完整皮肤无致敏作用,对豚鼠完整及破损皮肤均无刺激；延芍贴剂的镇痛效果确切。[结论]在脐中穴经皮给药贴剂研究中,所用基质与促透剂应进行最佳性筛选试验,确定二者与药物适宜性关系；应用体外透皮实验是筛选基质、促透皮吸收剂适宜的药动学方法；延芍贴膏剂脐中穴经皮给药具有安全性、有效性、稳定性和可控性更多还原

【Abstract】 [Objective] In order to clarify the scientific and the theoretical basis of the umbilical point to transdermal drug delivery, to establish the common technology and quality evaluation system of umbilical point to transdermal drug delivery and to provide the scientific basis for the creation morden prepration of umbilical point to transdermal drug delivery. [Method] We read documentation about umbilical point to transdermal drug delivery and research from the meridian, anatomy, physiology, clinical application, pharmaceutical pharmacy and drug percutaneous absorption theory. Respectively,white peony and the ethanol extract of corydalis herbal medicine as raw materials,use of the modern new excipient such as unsaturated fatty acid glyceride,cocoa butter,polyethylene glycol, glycerin-gelatin-water polo sharm as the substrate to fat-soluble Azone,water-soluble Azone and dimethyl sulfoxide were prepared to promote the transdermal absorbent paste paste, Franz diffusion cell simulation of the human body through the percutaneous absorption process, carried out process preparation study of different delivery systems; We take irritation test and allergic test to the guinea pig skin and make pharmacodynamic studies through the writhing and hot plate method. [Result] Yan Shao paste paste which uses glycerin- gelatin-water as the substrate and 3% fat-soluble Azone as penetration enhancer has the best effect of percutaneous absorption;Yan Shao paste paste has no allergic effect to the guinea pig intact skin and damaged skin;The effect of relieving pain of Yan Shao paste paste is recognized. [Conclusion] In the studies of the umbilical point to transdermal drug delivery the substrate and penetration should take filtration test to determine the suitablity relationship between them and the medicine;The use of extracorporal penetration experiment is a suitable pharmacokinetics method to filter the substrate and penetration enhancer;The umbilical point to transdermal drug delivery of Yan Shao paste paste has security,effectiveness,stability and controllability.更多还原