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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: As long-term use of levodopa in the treatment of Parkinson’s disease, its drug concentration fluctuations easily lead to dyskinesia, the purpose of this experiment is to prepare a small burst release, drug release concentration stable levodopa methyl ester microsphere preparation. Methods: The levodopa methyl ester was encapsulated in PLGA microspheres by double emulsion method. The drug entrapment efficiency and in vitro release behavior were studied by C18 reverse phase chromatography. Results: By adjusting the drug concentration and different polymer combinations, we chose a prescription with small release, high entrapment efficiency and slow release. Conclusion: L-dopa methyl ester encapsulated in PLGA can achieve the desired sustained-release effect, reduce the concentration fluctuations, and provide the basis for later pharmacodynamic experiments.