【作者】 王晓艳；

【导师】 王东凯；

【作者基本信息】 沈阳药科大学 ， 药剂学， 2004， 硕士

【摘要】 本文采用热融超声分散法和溶剂乳化法制备α—细辛脑固体脂质纳米粒(ARE-SLN)，对于制得的载药纳米粒进行以下研究：考察其各项物理化学性质；通过冷冻干燥和粉末包衣技术将纳米粒制备分别制备成冻干粉针和固体制剂；研究大鼠口服载药纳米粒后的药代动力学特征，以及载药纳米粒在大鼠各组织器官中的靶向作用。 建立了紫外分光光度法测定药物的包封率、表观溶解度和油水分配系数，方法简单，结果准确，以蒸馏水或无水乙醇为溶剂，在313nm处测定吸收度，经方法学验证，适用于该品体外控制；采用高效液相色谱法测定药物的含量和体外释放，分离效果好，准确快速，经方法学验证，适用于该品体外控制。同时还测定了原料药和脂质材料的熔点。 对于固体脂质纳米粒的制备，分别进行两种制备方法的研究：热融超声分散法和溶剂乳化法。首先进行了单因素试验考察，以制得的纳米粒胶体溶液的稳定性和包封率为指标，在单因素实验的基础上，采用正交设计进行优化，分别确定了这两种方法的最佳处方组成和制备工艺条件。 对所制得的纳米粒进行一系列理化性质的考察，简要描述了脂质纳米粒的形态以及特征，为最佳处方、制备工艺的确定、制剂的稳定性和质量的保证提供了依据：考察了纳米粒的外观形态，粒径分布、Zeta电位、pH、DSC扫描图谱、纳米粒混悬液的运动粘度、纳米粒包封率的变更多还原

【Abstract】 The main goal of this paper was to prepare α-Asarone-loaded solid lipid nanoparticles (ARE-SLN) by two method and to investigate the physico-chemical characteristics of them, drug pharmacokinetics, as well as tissue distribution in vivo relative to α-Asarone control solution.Ultraviolet (UV) spectrophotometry method was developed for determination of encapsulation efficiency, solubility and oil/water partition coefficient of α-Asarone; High-performance liquid chromatography (HPLC) method with UV detection was applied to detect content, drug release as well as the plasma concentration and the tissues concentration of α-Asarone in rats. The two analysis methods are precise, simple and reliable.Lipid (Monostearin) and surfactant were used to prepare ARE-SLN by heating-ultrasound divergence method and solvent-emulsion method respectively. With the criteria of encapsulation efficiency and deposited stability orthogonal design experiments were performed to optimize the conditions for the process.Many physico-chemical characteristics of ARE-SLN were investigated .The appearance and particle size distributions of the ARE-SLN were examined by transmission electron microscopy and laser diffraction, respectively. The average diameter of ARE-SLN is between 60～80 nm. The encapsulation efficiency was更多还原