| 摘要: |
| 目的制备载艾塞那肽的聚乳酸-羟基乙酸共聚物［poly (lactic-co-glycolicacid),PLGA］微球,并对其体外释药特性进行考察。方法以聚乳酸-羟基乙酸共聚物为载体,采用凝聚法(W/O/O)制备载艾塞那肽缓释注射微球,建立了高效液相色谱测定艾塞那肽含量的方法和微球中药物提取方法,考察微球粒径大小、外观、包封率、载药量等理化性质,并对微球体外释放特性进行了考察。结果微球球形较圆整,平均粒径为(51.2±1.97)μm,实际载药量为(4.50±0.13)%,包封率在(96.5±2.68)%, |
| 关键词: 艾塞那肽 微球体 聚乳酸-羟基乙酸共聚物 高压液相色谱法 体外释放 迟效制剂 |
| DOI：10.3724/SP.J.1008.2011.0768 |
| 投稿时间：2011-03-21修订日期：2011-07-01 |
| 基金项目: |
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| Preparation of sustained-release microspheres containing exenatide and their in vitro release |
| XUAN Ji-ming,GAO Jing,HUANG Jing-bin,LIN Ya-ling,LU Ying,ZHONG Yan-qiang* |
| (Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China) |
| Abstract: |
| [Abstract] Objective: To preparation exenatide loaded poly (lactic-co-glycolicacid) (PLGA) microspheres and to evaluate its release behavior in vitro. Methods: Exenatide PLGA microspheres were prepared by W/O/O method. The content and in vitro cumulative release was determined by a HPLC method, the physical and chemical characteristics of microspheres, including the mean diameter, morphology, drug entrapment efficiency and loading efficiency were evaluated. Results: The prepared microspheres were well-shaped, with mean diameter of (51.2±1.97)μm. The drug loading and encapsulation efficiency were (4.50±0.13)% and (88.6±0.73)%, respectively. The first day burst release was (13.19±1.39)%. The cumulative in vitro release was up to (88.6±0.73)% in 28 day. Conclusion: The exenatide can encapsulated in microspheres to yield a one-month continuous release using biodegradable polymers PLGA as the carrier material and the process is stable and reproducible. |
| Key words: Exenatide microspheres poly(D,L-lactide-co-glycolide) HPLC in vitro release |
