| 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 |
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| 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） |
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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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