左旋多巴甲酯缓释微球的研究

Research of Levodopa Methyl Ester-loaded Microspheres Delivery System

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。

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.