格列吡嗪壳聚糖-三聚磷酸钠pH敏感性微球的制备及性能研究

Preparation and properties evaluation for glipizide loaded CS-TPP pH sensitive microspheres

目的:以壳聚糖为载体,制备格列吡嗪壳聚糖-三聚磷酸钠pH敏感性微球,并对其性能进行研究。方法:采用正交试验设计法L9(34)优化处方组成及微球制备工艺,通过扫描电镜法、红外光谱法对微球的表面形态及内部结构进行表征,并对其体外释放性能进行研究。结果:最佳工艺条件下制得的微球形状圆整、表面光滑,平均包封率、载药量、粒径分别为75.17%,11.04%和50μm。此微球在模拟胃液中3 h,累积释放率达50%,转移到肠液中19 h后,累积释放率达80%。结论:该微球具有明显的pH敏感性和控释性能。

ORIECTIVE To prepare the pH sensitive glipizide loaded CS-TPP microspheres, and to investigate its properties of the microspheres. METHODS Chitosan was selected as carrier material. Glipizide loaded CS-TPP microspheres composition and preparation technology was optimized by orthogonality of L9（3^4 ）. The surface morphology and structure of the microsphere was characterized by scanning electron microscopy （SEM） and FTIR, respectively. Also, the microsphere release in vitro was determined. RESULTS Glipizide loaded microspheres under the optimum preparation conditions showed a round shape and smooth surface, and average encapsulation efficiency, loading efficiency and particle diameter were 75.17 %, 11.04 % and 50 μm, respectively. In addition, the sequential release amount of glipizide from the hydrogel microspheres in SGF was 50 % for 3 h, and then moved to SIF, this value approached 80% for 24 h. CONCLUSION The method of the preparation was successful, and the microspheres occupied obviously pH sensitivety and controlled release effect in vitro.