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背景:口服胰岛素易被胃酸及胃肠道内的各种酶降解,难以透过胃肠道上皮细胞膜。针剂形式注射胰岛素也需要至少间隔36h注射1次。目的:制备口服胰岛素缓释微球。设计、时间及地点:对比观察实验,于2003-09/2004-12在南京信息工程大学药物化学实验室完成。材料:胰岛素由南京生化制药厂提供。方法:采用液中干燥法制备微球,利用在一定pH值条件下能溶解的丙烯酸树脂作为药物载体,得到包封胰岛素的丙烯酸树脂微球。主要观察指标:扫描电镜观察口服胰岛素微球形态及粒径的大小。紫外分光光度法测定胰岛素的含量,考察内相聚合物浓度和搅拌速度对微球粒径和药物包封率的影响。结果:扫描电镜下微球较圆整,表面较粗糙,球表面有许多小孔。随着搅拌速度的增加和内相聚合物浓度的减小,微球粒径减小,药物包封率有所增加。随着起始投药量的增加,微球中的含药量也相应增加,但投药量的高低对药物的包封率无显著影响。结论:液中干燥法能较好地制备口服胰岛素缓释微球。
Background: Oral insulin is easily degraded by gastric acid and various enzymes in the gastrointestinal tract, making it difficult to penetrate the gastrointestinal epithelial cell membrane. Injection of insulin also requires at least 36h intervals injection. Objective: To prepare oral insulin sustained-release microspheres. DESIGN, TIME AND SETTING: The comparative observation experiment was performed at the Pharmaceutical Chemistry Laboratory of Nanjing University of Information Science and Technology from September 2003 to December 2004. Materials: Insulin was provided by Nanjing Biochemical Pharmaceutical Factory. Methods: Microspheres were prepared by liquid drying method. Acrylic resin encapsulated with insulin was obtained by using acrylic resin which can dissolve under certain pH value as drug carrier. MAIN OUTCOME MEASURES: Morphology and size of oral insulin microspheres were observed by scanning electron microscopy. The content of insulin was measured by ultraviolet spectrophotometry. The influences of the concentration of the internal phase polymer and stirring speed on the particle size and encapsulation efficiency of the microspheres were investigated. Results: The microspheres under SEM were more rounded and the surface was rough. There were many small holes on the surface of the ball. With the increase of the stirring speed and the reduction of the internal polymer concentration, the particle size of the microspheres decreased and the drug entrapment efficiency increased. With the increase of the initial dosage, the drug content in the microspheres increased accordingly, but the dosage of the drug had no significant effect on the encapsulation efficiency of the drug. Conclusion: The liquid drying method can be better prepared oral sustained-release insulin microspheres.