文档介绍：广东药学院硕士研究生论文 III 中文摘要本课题选择天然大分子材料明胶(Gelatin)为成球材料,制备可用于关节腔注射的载转化生长因子-? 1(TGF-? 1)缓释微球,并研究了其体外释药特性。本课题采用乳化-交联法制备空白明胶微球,对明胶浓度、乳化剂用量、丙酮用量、油水比例、转速、乳化时间、固化剂及固化时间等处方工艺因素进行了单因素考察, 并根据单因素考察结果设计正交试验,以微球的形态、粒径及跨距为评价指标,筛选出明胶微球最优制备工艺。以明胶微球最优处方工艺制备微球用于TGF-? 1载药,对载药方法及工艺影响因素作了考察。并考察了各处方载药量、包封率及释放行为。本课题采用光学显微镜,在线观察软件及SPSS统计软件等对微球各方面性质进行考察,获得最优处方工艺为:明胶浓度为10%、乳化剂用量为5%、丙酮用量为3 ml、油水比例为3:1、转速为1000 rpm、乳化时间为13 min、固化剂为37%甲醛、固化时间为18 h。结果表明微球球形圆整,表面光滑,分散均匀, μm,。建立了TGF-? 1的含量的ELISA检测分析方法,获得ELISA法检测TGF-? 1含量的标准曲线,并对其专属性、精密度、重复性及回收率进行考察。ELISA法检测TGF-? 1 含量灵敏度好、专属性高。采用振摇-离心的载药方法,获得微球包封率达到98%以上,释放时间能够达到4天以上。本课题对TGF-? 1明胶微球的制备及载药方法进行了初步的考察,获得微球性能良好,工艺稳定,重现性好,并表现出制备成缓释制剂的潜力,有望开发为新药。关键词:TGF-? 1;明胶微球;ELISA 广东药学院硕士研究生论文 V Abstract Preparation of TGF-? 1 Loaded Gelatin Microspheres Student: Shi Jingyuan Major: Pharmaceutics Tutor: Chen Yanzhong This study focused at the potential of transforming growth factor ? 1(TGF-? 1) loaded gelatin microspheres to treat Rheumatoid Arthritis (RA). First, we studied the feasibility of the plan in theory. Then we prepared microspheres by emulsification cross-linking method. We researched fundamental preparing conditions such as concentration of gelatin, volume of emulsifier, volume of acetone, W/O radio, rotate speed, emulsification time, cross-linking agent and cross-linking independent variables including volume of emulsifier, volume of acetone, volume of formaldehyde in prior cross-linking were optimized by orthogonal designs. Using the optimized method prepared TGF-? 1gelatin microspheres and researched drug loading method. The results of drug loading,entrapment efficiency and release profiles were obtained. The physical characters of microspheres were evaluated by optical microscope and measured by online software named Optoro2008. The optimized formulation and procedure including: concentration of gelatin is 10%, volume of emulsifier is 5%, volume of acetone is 3 ml, W/O radio is 3:1, rotate speed is 1000 rpm, emulsific