氧氟沙星明胶微球的制备工艺研究

摘要

目的：研究制备氧氟沙星明胶微球的最佳工艺条件。方法以明胶为载体，液体石蜡为油相，Span80为乳化剂，戊二醛为交联剂，采用乳化交联法制备氧氟沙星明胶微球。采用紫外分光光度法测定微球中氧氟沙星的载药量和包封率。考察明胶质量分数、油水相体积比、明胶与氧氟沙星质量比、Span80体积分数对载药量、包封率的影响。以载药量、包封率的总和为评价指标，针对上述4个因素用L9(34)表正交试验设计法进行实验，获得最佳配方比例。结果氧氟沙星明胶微球分别在明胶质量分数20%、油水相体积比为3.5∶1、明胶与氧氟沙星质量比1∶1、Span80体积分数2.5%时，各自载药量、包封率的综合评价指标较高。正交设计证实上述条件下制备工艺最佳。结论本制备工艺稳定可行，氧氟沙星明胶微球的载药量和包封率可达到约80％。%Objective To study the optimum condition of preparing ofloxaxcin gelatin microspheres. Methods Oflox⁃axcin gelatin microspheres were manufactured using the emulsion chemical-cross linking method and gelatin was employed as carrier, liquid paraffin as oil phase, Span80 as emulsifier, . The loading capability and entrapment efficiency of the ofloxax⁃cin gelatin microspheres were determined by UV Spectrophotometry. The effect of gelatin concentration, oil/water volume ra⁃tio, gelatin/ofloxaxcin mass ratio and volume fraction of span80 on drug loading capability and entrapment efficiency were in⁃vestigated. The optimum proportions of each component was obtained by L9 (34) orthogonal test, based on the above 4 factors, using sum of drug loading capability and entrapment efficiency as evaluation index. Results The optimum condition for manufacturing high quality ofloxaxcin gelatin microspheres used 20%of gelatin concentration,water/oil volume ratio at 3.5∶1, gelatin/ofloxaxcin mass ratio at 1∶1, the span 80 volume fraction of 2.5%. Conclusion Drug loading capability and entrap⁃ment efficiency of the ofloxaxcin gelatin microspheres reached 80%using this manufacture technology therefore the prepara⁃tion was stable and feasible.