吸附和包埋法制备洛美沙星淀粉微球及其体外释放比较研究

Preparation of Lomefloxacin Starch Microspheres by Incubation Absorption and Entrapping and Their Comparative Study on Their Releases in Vitro

关键词:  可降解淀粉微球  盐酸洛美沙星  吸附载药法  包埋载药法  体外释放

Key words:  degradable starch microspheres  lomefloxacin  incubation absorption  entrapping  drug release in vitro

摘要:

目的 制备盐酸洛美沙星淀粉微球，并对其体外释药模式进行研究。方法 以盐酸洛美沙星为模型药物，采用吸附载药法和包埋载药法制备了载药淀粉微球，通过测定微球载药量、包封率和在不同的释放介质中的体外释放情况，对上述2种方法制备的载药微球进行质量评价。结果 吸附法制备的载药微球的平均载药量为14.54 µg·mg^-1，药物包封率为39.72%；而包埋载药法制备的淀粉微球的平均载药量为19.32 µg·mg^-1，药物包封率为48.95%。体外释药特性研究表明它们具有缓释特性，其中包埋载药法制备的淀粉微球比吸附载药法制备的淀粉微球有更好的缓释能力，在不同的释放介质中释药曲线也有所不同，在模拟胃液中累计释药量只能得到70%；而在模拟肠液中累计释药量能达到80%以上。结论 吸附载药法和包埋载药法制备的载药淀粉微球都具有缓释作用，但后者体外释药具有更明显的缓释效果。

Abstract:

OBJECTIVES To prepare lomefloxacin degradable starch microspheres (LFLX-DSMs) and to investigate the drug release behavior in vitro. METHODS Lomefloxacin is used as the model drug. LFLX-DSMs were prepared by incubation absorption and entrapping respectively, the performance of which was evaluated by drug-loading, encapsulation efficiency and the drug releasing of LFLX-DSMs in vitro. RESULTS The drug-loading is (14.54±0.87)μg·mg^-1 and encapsulation efficiency is (39.72±0.65)% by incubation absorption, while the drug-loading is (19.32±0.68)μg·mg^-1 and encapsulation efficiency is (48.95±0.73)% by entrapping. The results indicate that LFLX-DSMs had a slow release of LFLX in vitro, and the releasing effect of entrapping is better than that of incubation absorption. The drug release curve of DSMs in the different media were not the same, the drug released less than 70% in artificial gastric juice and more than 80% in artificial intestinal juice. CONCLUSION Both of the methods had a slow release of LFLX in vitro, but the better releasing effect had been achieved by entrapping.