中国组织工程研究

中国组织工程研究 ›› 2012, Vol. 16 ›› Issue (12): 2212-2216.doi: 10.3969/j.issn.1673-8225.2012.12.028

• 生物材料基础实验 basic experiments of biomaterials • 上一篇    下一篇

吲哚美辛微球的制备及其包封率和释放性能***★

高  颖1，吴艺君1，南开辉1, 2，李文生1，温  俊3   

  1. 1温州医学院附属眼视光医院，浙江省温州市  325027；2温州医学院生物医学工程研究院，浙江省温州市   325027；3温州医学院药学院，浙江省温州市  325027
  • 收稿日期:2011-09-19 修回日期:2011-10-23 出版日期:2012-03-18 发布日期:2012-03-18
  • 通讯作者: 温俊，副教授，温州医学院药学院，浙江省温州市 325027 terwj2004@ yahoo.com.cn
  • 作者简介:高颖★，女，1987年生，安徽省肥西县人，汉族，温州医学院在读硕士，主要从事生物材料，眼科药物载体及眼科疾病治疗等方面的研究。gaoying.1987517@163.com
  • 基金资助:

    浙江省大学生科技创新活动计划(新苗人才计划)资助项目(2010R413051)，课题名称：吲哚美辛眼用缓释微球的制备；浙江省医药卫生科学研究基金资助项目(2009A138)，课题名称：吲哚美辛缓释植入体防治增生性玻璃体视网膜病变的实验研究；温州市科技局面上项目资助(Y20090014)，课题名称：吲哚美辛缓释植入体的制备及对兔眼增生性玻璃体视网膜病变防治作用研究。

Preparation, entrapment efficiency, and release property of indomethacin microspheres

Gao Ying1, Wu Yi-jun1, Nan Kai-hui1, 2, Li Wen-sheng1, Wen Jun3   

  1. 1School of Ophthalmology and Optometry, Wenzhou Medical College, Wenzhou  325027, Zhejiang Province, China; 2Biomedical Engineering Academy, Wenzhou Medical College, Wenzhou  325027, Zhejiang Province, China; 3Pharmacy School of Wenzhou Medical College, Wenzhou  325027, Zhejiang Province, China
  • Received:2011-09-19 Revised:2011-10-23 Online:2012-03-18 Published:2012-03-18
  • Contact: author: Wen Jun, Associate professor, Pharmacy School of Wenzhou Medical College, Wenzhou 325027, Zhejiang Province, China terwj2004@ yahoo.com.cn
  • About author:Gao Ying★, Studying for master’s degree, School of Ophthalmology and Optometry, Wenzhou Medical College, Wenzhou 325027, China gaoying.1987517@ 163.com
  • Supported by:

    Scientific and Technological Innovation Project of Zhejiang University, No. 2010R413051*; Research Foundation of Medicine and Health of Zhejiang Province, 2009A138*; General Foundation of Science and Technology Agency of Wenzhou, No. Y20090014*

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摘要：

背景：吲哚美辛在眼内半衰期短，需要多次给药才能达到治疗作用。
目的：制备吲哚美辛微球，并分析其包封率及缓释性能。
方法：选择安全性好的聚乳酸-羟基乙酸共聚物和聚丙烯酸树脂类两种共聚物作为载体材料，以乳化溶剂挥发法制备含吲哚美辛微球，分析不同有机溶剂(二氯甲烷、丙酮)、不同载体材料比例、不同pH值及不同渗透压因素对微球包封率和体外释放性能的影响。
结果与结论：微球表面光滑圆整，无孔，粒径分布表现出多分散性，粒径2.0~3.0 μm。制备过程中发现，有机溶剂使用二氯甲烷、载体材料聚乳酸-羟基乙酸共聚物：聚丙烯酸树脂类的质量比例越小、水相中pH值越低、渗透压越低，载药微球的包封率越大。在聚乳酸-羟基乙酸共聚物：聚丙烯酸树脂类的质量比为1∶3时，包封率最高，体外释放速率最慢。
关键词：吲哚美辛；聚乳酸-羟基乙酸共聚物；聚丙烯酸树脂类；微球；乳化溶剂挥发法
doi:10.3969/j.issn.1673-8225.2012.12.028

关键词: 吲哚美辛, 聚乳酸-羟基乙酸共聚物, 聚丙烯酸树脂类, 微球, 乳化溶剂挥发法

Abstract:

BACKGROUND: Indomethacin requires multiple doses to achieve treatment effect because of its short half-life in ocular.
OBJECTIVE: To prepare indomethacin microspheres and analyze its entrapment efficiency and release property. 
METHODS: Indomethacin microspheres were prepared by emulsion solvent evaporation using poly lactic acid-glycolic acid copolymer and polyacrylic acid resin based on their good safety. The influences of preparation parameters on encapsulation efficiency and release property were investigated, such as different organic solvent (dichlormethane, acetone), different proportions of polymer, different pH values and osmotic pressures.
RESULTS AND CONCLUSION: The microspheres were spherical shape with a smooth and imperforation surface, and had fine dispersibility at a diameter of 2-3 μm. The dichloromethane, lower weight of polyacrylic acid resin, lower pH and osmotic pressure in water medium could result in higher entrapment efficiency. The entrapment efficiency was the highest and the release rate was the slowest at 1:3 of poly lactic acid-glycolic acid copolymer and polyacrylic acid resin.

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