文章摘要
任甜甜郑瑞媛胡振华蔡云鹏陈晓静朱涵蕾袁伟恩.左旋多巴甲酯缓释微球的研究[J].,2011,11(11):2034-2036
左旋多巴甲酯缓释微球的研究
Research of Levodopa Methyl Ester-loaded Microspheres Delivery System
  
DOI:
中文关键词: 左旋多巴甲酯  PLGA 微球  缓释  帕金森氏病  异动症
英文关键词: LDME  PLGA microspheres  Sustained release  Parkinson's disease  Levodopa-induced dyskinesia
基金项目:国家重大专项-" 重大新药创制" 科技重大专项-创新药物研究开发技术平台(2009ZX09310-007) 上海科委项目(No.0952nm03700 和No.1052nm03900)和上海交通大学大学生创新项目(IPP2090)
作者单位
任甜甜郑瑞媛胡振华蔡云鹏陈晓静朱涵蕾袁伟恩 上海交通大学 
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中文摘要:
      目的:由于长期服用左旋多巴治疗帕金森病,其药物浓度波动刺激易引起异动症,本实验旨在制备突释小,药物释放浓度稳 定的左旋多巴甲酯微球制剂。方法:将左旋多巴甲酯用复乳法包裹于PLGA 微球内,采用C18 反相色谱研究药物包封率和体外释 放行为。结果:通过调节药物浓度和不同高分子组合筛选出突释小,包封率高且缓慢释放的处方。结论:左旋多巴甲酯包裹于 PLGA 能实现理想的缓释效果,降低药物浓度波动,为后期药效学实验提供基础。
英文摘要:
      Objective: Chronic administration of levodopa in the treatment of PD leads to debilitated involuntary movements, we aimed to prepare levodopa methyl ester-loaded sustained release microspheres without initial burst. Methods: Levodopa methyl ester (LDME) were microencapsulated into PLGA microspheres by multiple emulsion technique. The encapsulation efficiency and vitro release of microspheres were detected using HPLC system equipped with a C18 reverse column. Results: By adjusting LDME concentration and different polymer combinations, we achieved microspheres with high encapsulation efficiency, low initial burst and sustained release. Conclusions: LDME would achieve sustained release while encapsulated into PLGA microspheres, which provided a basis for later pharmacodynamic study.
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