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].现代生物医学进展英文版,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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