左旋多巴微囊制备工艺的研究

目的以乙基纤维素为囊材,优选左旋多巴微囊的制备工艺。方法以微囊的包封率及载药量为评价指标,采用正交实验优选左旋多巴微囊液中干燥法制备工艺条件,并对制备的微囊进行质量检查。结果优选出的制备工艺为:囊材与药量比例为0.6∶1.4,油水相比例为105∶30,PVP量为0.2g,验证实验表明,优化工艺所制左旋多巴微囊的平均载药量为54.94%,平均包封率为89.2%。质量检查结果表明,微囊外观圆整且无粘连现象,大部分微囊的粒径分布在300～600μm范围内。优选出的左旋多巴微囊在体外具有明显的缓释效果。结论采用液中干燥法制备左旋多巴微囊,工艺稳定可靠,操作简便,工艺条件合理、可行。

Study on the preparation of Levodopa Microcapsules

Objective To optimize the preparation method of levodopa（LD） ethylcellulose（EC） microcapsules.Method LD was microcapsulated by the method of intra-liquid desiccation.The index of drug-loading rate and entrapment rate were selected as indexes,and the preparing of LD microcapsules was optimized by the orthogonal design.Results The optimized preparing way of LD microcapsules was as follows：the weight rate of EC and LD was 0.6∶1.4,the rate of oil phase and water phase was 105∶30 and the weight of PVP was 0.2 g.The result of verification test showed that the drug-loading rate of optimized LD microcapsules was 54.94% and the entrapment rate was 89.2%.The results of quality inspection showed that the appearance of LD microcapsules was rounding and kept from sticking.The range of particle size of LD microcapsules was 300-600 μm.Microcapsules release in vitro had a sustained release characteristics.Conclusion The preparation method of LD is stable and reliable.The condition of preparation is reasonable and feasible.