包载尼莫地平的聚乳酸-聚乙二醇嵌段共聚物纳米粒的制备和质量评价

目的制备尼莫地平纳米粒的粉针剂，以期改善尼莫地平难溶于水而导致易析出晶体的问题以及其制剂中乙醇引起血管刺激的毒副作用。方法以聚乳酸、聚乙二醇嵌段共聚物作为载体，用溶剂挥发法制备载药纳米粒水分散体系及其冻干粉针．并评价其粒径、Zeta电位、包封率、载药量、形态和冻干粉针的再分散性等性能。结果制备了136nm载药纳米粒的冻干粉针，Zeta电位为-29．90mV，包封率为67．9％，载药量为6．17％，冻干再分散情况良好。结论所制备的尼莫地平纳米粒基本解决了原有制剂药物溶解性差，易析出晶体的问题，避免使用有机溶剂和有副作用表面活性剂的应用。

Preparation of nimodipine-loaded PLEG copolymer nanoparticles and quality evaluation

Objective To improve the poor water-solubility of nimodipine,nimodipine-loaded PLEG copotymer nanoparticles were prepared to avoid the sedimentation of its crystal from water, which could also shun the blood vessel stimulation caused by ethanol,a cosolvent,in the injection. Methods Solvent evaporation method was used to prepare water-dispersing nimodipine-loaded nanoparticles, whose lyophilized powder was further prepared, with PLEG2000 as drug carrier. Particle size, Zeta potential, embedding ratio, drug loading, shape and redispersion ability of the tyophitized powder were determined. Results Concerning the tyophilized nanoparticle powders, the particle sizes were 136nm,the Zeta potentials were -29.90mV, the embedding ratio was 67.9 % and the drug loading was 6.17%. Conclusion Prepared nimodipine-loaded nanoparticles solved the problem of poor water-solubility of nimodipine basically. It also avoided the recrystallization process of the drug and reduced the blood vessel stimulation caused by ethanol in the injection.