胃溶型烟酸微囊的制备及优化筛选

Preparation and optimized screening of gastric- soluble nicotinic acid microcapsules

烟酸又称抗癞皮病因子,是机体必需的13种维生素之一。然而,烟酸本身味苦,限制了其在临床上的应用。为了克服烟酸的苦味,试验采用液中干燥法研制烟酸微囊;并以包封率及载药量为指标,考察溶剂、囊材、乳化剂、抗黏剂的用量对烟酸微囊的影响,以确定最佳制备方案。结果表明:应用优化工艺制备的烟酸微囊的载药量为29.43%,包封率为65.33%,烟酸微囊在p H值为1.0,2.0的溶出介质中10 min内溶出度超过70%。说明采用液中干燥法制备烟酸微囊,操作简便,载药量高,具有胃溶特性,应用前景良好。

Nicotinic acid which is also known as antipellagra factor is one of the 13 kinds of essential vitamins in the body. However, nicotinic acid is limited in clinic application because of its bitterness. To overcome the bitterness of nicotinic acid, nicotinic acid microcapsules were de- veloped by in - liquid drying method. The effects of the contents of solvents, capsules shell materials, emulsifiers, and antiadherents on the nicotinic acid microcapsules were investigated to determine the optimum preparation scheme using encapsulation efficiency and drug loadings as indexes. The results showed that the drug loadings of nicotinic acid microcapsules prepared using the optimization process using the optimization process was 29.43 % while the encapsulation rate was 65.33 %. The dissolution rates of nicotinic acid microcapsules in the pH 1.0 and pH 2.0 dissolution media were both more than 70 % within 10 min. The results indicate that using the in - liquid drying method to prepare nicotin- ic acid microcapsules has the advantages of simple operation and high drug loadings. The prepared nicotinic acid microcapsules have the charac- teristics of gastric solubility, having a good application prospect.