【作者】 于晓佳；

【导师】 贾伟；

【作者基本信息】 天津大学 ， 药物化学， 2005， 硕士

【摘要】 本论文的研究目的在于将传统的口服金铃子散剂改制为便于使用的软膏剂及外用贴剂。采用正交实验法,以制剂的稳定性及外观、性状等作为考察指标,对金铃子散软膏剂、巴布剂的基质进行实验研究,确定软膏剂、巴布剂最适宜的基质组成。软膏剂最优的基质组成及工艺为凡士林10.0g、硬脂酸7.0g、液体石蜡6.0g、甘油5.0g、三乙醇胺2.0g,于75℃采用乳化法制备;巴布剂的最优基质组成为明胶16.0g,聚乙烯醇(PVA)4.0g,聚丙烯酸钠(PANa)10.0g,聚乙烯吡咯烷酮( PVP) 4.0g,甘油10.0g,丙二醇10.0g,高岭土6.0g。采用HPLC法,以药物中的有效成分延胡索乙素(Tetrahydropamatine,THP)为检测指标,建立了软膏剂提取液、巴布剂提取液和透皮接收液的分析方法,具体为色谱柱: ODSC18, 5μm, 250×0.46mm;流动相:甲醇-0.25%Na2HPO4水溶液(69:31);流速:1.0ml·min-1;检测波长为280nm;柱温:25℃,线性形范围为0.06～120μg·ml-1。通过体外扩散池法,以生理盐水为接收液,考察促透剂对药物透皮吸收的影响,对处方进行进一步筛选。促透剂并没有起到明显的促进药物渗透的作用。金铃子散可改制成软膏剂及巴布剂,按上述方法制备的软膏剂、巴布剂符合中国药典2000版有关软膏剂及巴布剂的规定。更多还原

【Abstract】 In this paper, preparation of Jinlingzi cream and Jinlingzi cataplasmwas studied.We used orthogonal design method to determine matrixcomposition, and use the stability and appearance properties of thecream and cataplasm to evaluate them. The optimum matrixcomposition and technology of cream were: vaseline 10.0g, stearicacid 7.0g, liquid paraffin 6.0g, glycerin 5.0g, triethanolamine 2.0g,emulsify temperature 75 ℃. The optimum matrix composition ofcataplasm were: Gelatin 16.0g, PVA 4.0g, PANa 10.0g, PVP 4.0g,glycerin 10.0g, propylene-glycol 10.0g, Kaolin 6.0g.To determine Tetrahydropalmatine in cream and cataplasm and itspermeation through pretreated mouse skin, HPLC method wasdeveloped, using reverse phase C18 colunm, the mobile phase ofwhich consisted of 0.25% disodium hydrogen phosphate andmethanol ( 31:69) with a UV detector at 280nm. The linearity ofstandard curve for Tetrahydropalmatine to be acceptable (r=0.999996)over the range 0.06～120μg·ml-1.By applying conventional drug delivery method, penetrationenhancers that affect the controlled released Tetrahydropalmatine(THP) delivery system have been investigated. Results indicated thatno penetration enhancer could effectively enhance the skinpermeation of Tetrahydropalmatine.The two dosage forms, cream & cataplasm, prepared by the optimizedprocess were in good compliance with the stipulation of ChinesePharmacopoeia( 2000) .更多还原