胰岛素聚β-羟基丁酸酯微球体外性质的研究  

In vitro Charaterization of Insulin-Loaded Poly(β-hydroxybutyrate)Microspheres

作　　者：庞伟 杨红[2] 陆彬[2] 

机构地区：[1]甘孜藏族自治州藏医院,四川康定626000 [2]四川大学华西药学院

出　　处：《中国药师》2008年第10期1138-1140,共3页China Pharmacist

基　　金：国家教委博士点基金项目(编号9504113)

摘　　要：目的:以液中干燥法优化制得到的胰岛素聚β-羟基丁酸酯微球作为研究对象,考察微球的体外相关性质。方法:通过光学显微镜观察微球表面形态;用固定漏斗法测定微球的流动性;通过重量法考察微球的吸湿性;在冷藏和室温条件下,考察微球的初步稳定性;通过体外释放试验,考察微球中药物体外释放特点。结果:微球表面光滑,外观呈球形,流动性良好,临界相对湿度为95.09%,在考察条件下,微球的外观及微球的载药量没有显著变化;与原药胰岛素相比,微球中药物体外释放t_(1/2)延长6倍多,表现出一级动力学规律,释药后微球形态改变。结论:微球的缓释作用明显,微球释放药物后,发生了明显的降解。Objective： To investigate the in vitro properties of insulin-poly （β-hydroxybutyrate） microspheres prepared by in-liquid drying method under optimized conditions. Methods： The morphology and appearance of the microspheres were examined by optical microscopy, the fluidity by fixed funnel method, the hygroscopicity by gravimetric method, the preliminary stability by storing under refrigerated and room temperature conditions, and the in vitro release profile by observing the insulin release from the microspheres. Results： The microspheres looked spherical with smooth surface and good fluidity. The critical relative humidity of the microspheres was 95.09%. The microspheres which had been stored at 4℃ and room temperature for 3 months showed no detectable changes in the shape, fluidity and drug loading ratio. The release profile was in accord with the first order kinetics with a release t1/2 7 times longer than insulin solution, and the appearance of the microshpers changed after drug release. Conclusion： Compared with insulin, the microspheres showed obvious sustained release characteristic and degraded obviously after drug release.

关 键 词：胰岛素 聚Β-羟基丁酸酯 微球 体外释放 降解 

分 类 号：R944.9[医药卫生—药剂学]