摘要
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 easy to be degradated by hydrochloric acid in gastric juice and the enzyme which exists in stomach and intestines, while it is difficult to through the epithelium cell membrane of gastrointestinal. Even a lasting-long injection is taken, and it still needs an injection once 36 hours. OBJECTIVE： To prepare oral insulin sustained-release microspheres. DESIGN, TIME AND SETTING： Contrast observation which was carried out at the Laboratory of Medical Chemistry of Nanjing Information Engineering University from September 2003 to December 2004. MATERIALS： Insulin was provided by Nanjing Medicinal Factory of Bio-Chemistry. METHODS： A new method to prepare the microsphere, i.e., drying through liquid phase was adopted with the special pH and the acrylic acid polymer which could be dissolved as the medicine＇s cartier of the sustained-release microphere. MAIN OUTCOME MEASURES： The effects of polymer concentration and agitation rates on size of microspberes and drug incorporation efficiency were studied by scanning electronic microscopy （SEM） and ultraviolet-spectrophotometry. RESULTS： The temperature, drug payloads and the content of emulsifier played important effects on microspheres formation. The mean diameter of microspheres decreased with increasing in stirring rate and decreasing in polymer concentration, and drug loading efficiency increased with increasing in stirring rate. CONCLUSION： Insulin-loaded polyacrylate sustained-release microspheres is prepared preferably.
出处
《中国组织工程研究与临床康复》
CAS
CSCD
北大核心
2008年第36期7179-7182,共4页
Journal of Clinical Rehabilitative Tissue Engineering Research
