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索拉非尼-Eudragit RS 纳米粒的制备及理化性质研究
Preparation and in vitro Drug Release of Sorafenib-Eudragit RS Nanoparticles
投稿时间:2014-10-23  修订日期:2014-12-31
DOI:
中文关键词:  索拉非尼;Eudragit RS100;纳米粒;溶剂-非溶剂法  优化;体外释放
英文关键词:Sorafenib  Eudragit RS100  Nanoparticles  Solvent-nonsolvent method  Optimization  In vitro release
基金项目:湖北省自然科学基金项目(编号:2012FKB04439)
作者单位
贾炜 武汉大学人民医院药学部 武汉 430060 
张洪 武汉大学人民医院药学部 
张英 武汉大学人民医院药学部 
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中文摘要:
      摘 要 目的: 制备索拉非尼-Eudragit RS 纳米粒(sorafenib-Eudragit RS nanoparticles,S-E NPs) ,优选制备处方及初步探索其理化性质。方法: 溶剂 非溶剂法制备索拉非尼 Eudragit RS 纳米粒,采用单因素试验研究溶剂、稳定剂类型、载体比例、有机相水相比例对纳米粒理化性质的影响。通过粒径和Zeta电位、形貌观察、体外释药考察对其进行质量评价。结果:优选处方制备的索拉非尼 Eudragit RS 纳米粒的平均粒径为(86.72±3.71) nm,多相分散系数(PDI)为(0.200±0.032),Zeta 电位为(36.6±0.3) mV,纳米粒呈球形且分布均匀;体外释放符合 Weibull 模型(r=0.966 9)。结论: 溶剂 非溶剂法适用于索拉非尼 Eudragit RS 纳米粒的制备,所制备的纳米粒粒径较小,分布均匀,形态规则完整,具有明显缓释作用。
英文摘要:
      ABSTRACT Objective: To prepare and optimize sorafenib Eudragit RS nanoparticles (S-E NPs) and investigate the physicochemical properties. Methods: S-E NPs were prepared by a solvent nonsolvent method. Single factor experiments were used to research the effect of solvent, stabilizer type, carrier ratio and the proportions of water phase and organic phase on the physicochemical properties of S-E NPs. S-E NPs were evaluated by the particle size, zeta potential and morphology, and the in vitro drug release of S-E NPs was studied using dialysis technology.Results: The mean size was(86.72±3.71)nm, the PDI and zeta potential was (0.20±0.032) and (36.6±0.3) mV,respectively, S-E NPs showed spherical shape with uniform distribution. The drug release in vitro was accorded with a Weibull equation. Conclusion:The solvent nonsolvent method is appropriate for the preparation of S-E NPs. The nanoparticles have small particle size, uniform distribution, regular morphology and significant sustained release property.
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