反溶剂法制备叶黄素酯纳米粒

发布时间：2018-06-20 17:57

  本文选题：叶黄素酯 + 纳米粒　； 参考：《中草药》2017年14期

【摘要】：目的优化叶黄素酯(LE)纳米粒(NPs)的制备工艺,并对其水溶性的改善程度进行测试。方法以四氢呋喃为溶剂,去离子水为反溶剂,泊洛沙姆188作为表面活性剂,通过反溶剂法制备LE-NPs,采用单因素实验设计法优化LE-NPs制备工艺。并综合利用扫描电子显微镜、激光粒度仪、X射线衍射、差示扫描量热法等分析方法对获得的LE-NPs理化性质进行表征;采用气相色谱(GC)进行溶剂残留测定;并进行了体外溶出对比实验。结果 LE-NPs的最优制备条件为沉积时间10 min,叶黄素酯质量浓度50 mg/mL,溶剂反溶剂体积比为1∶7,泊洛沙姆188质量分数0.5%,搅拌速率950 r/min,沉积温度25℃;所得LE-NPs为球形,平均粒径为164 nm,其中四氢呋喃残留量为344.3μg/g,低于人用药物注册技术要求国际协调会(ICH)要求的最低标准(0.780 mg/g);在人工胃液环境中LE-NPs的饱和溶解度和溶出速率分别是原药的2.91倍和9.65倍。结论反溶剂法制备的LE-NPs具有较好水溶性,在口服制剂中具有潜在的用途。
[Abstract]:Objective to optimize the preparation process of lutein Ester (LEL) nanoparticles (NPs) and to test the improvement of its water solubility. Methods LE-NPs were prepared by using tetrahydrofuran as solvent, deionized water as antisolvent and Poloxamer 188 as surfactant. The preparation process of LE-NPs was optimized by single factor experimental design. The physical and chemical properties of LE-NPs were characterized by scanning electron microscope (SEM), laser particle size analyzer (LE-NPs), X-ray diffraction (XRD) and differential scanning calorimetry (DSC). A comparative experiment of dissolution in vitro was carried out. Results the optimum preparation conditions of LE-NPs were as follows: deposition time 10 min, lutein ester concentration 50 mg / mL, solvent antisolvent volume ratio 1: 7, Poloxamer 188 mass fraction 0.5, stirring rate 950 rpm, deposition temperature 25 鈩，

本文编号：2045187