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.pdfVIP

医药2007年I1月第l4卷第 11期 Chin J Prim Med—Ph—arm， ! !! ：! ：!! · 1767 · 包载尼莫地平的聚乳酸一聚乙二醇嵌段共聚物 纳米粒的制备和质量评价 范 盈 周 辰 刘文胜 【摘要】 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136 nm载药纳米粒的冻干粉针，Zeta电位为一29．90 mV，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。 【关键词】纳米技术；聚乙烯二醇类；尼莫地平 Preparation of nimodipine—loaded PLEG copolymer nanoparticles and quality evaluation FAN Ying．ZHOU Cken．L，U Wen—sheng．School oJ Chemical Biolog3·and Pharmaceutica!Sciences．Capital University of Medical iences，Beijing 100069，China 【Abstract】 Objective To improve the poor water—solubility of nimodipine，nimodipine．1oaded PLEG copoty— met nanoparticles wcrc prepared to avoid the sedimentation of its crystal from water．which could also shun the blood ve~el stimulation caused by ethanol，a cosolvent．in the injection．Methods Solvent evaporation method was used to prepare water—dispersing nimodipine—loaded nanoparticles，whose lyophilized powderwas furtherprepared，with PLEG2000 as drug carrier Particle size．Zeta potentia1．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一29 90mV．the embedding ratio was 67．9％ and the drug loading was 6 1 7％ Conclusion Prepared nimodipine．1oaded nanoparticles solved the problem of poor water—solubility of ni— modipine basically．It also avoided the recrystal1ization process of the drug and reduced the blood vessel stimulation caused by ethanol in the injection． 【Key words】 Nanotechnology；Polyethy lene glycols；Nimodipine 尼莫地平已有片剂、胶囊剂和注射剂等市售剂 1．1 试验设备与试剂 FD一1E型冷冻干燥机(北京 型，因其肝脏首过效应严重、半衰期短且口服生物利 德天佑科技发展有限公司)，236HK型高速离心机 用度低，故临床上广泛使用其注射液。由于尼莫地