洛莫司汀-碘海醇复方脂质体的制备及包封率测定.PDFVIP

洛莫司汀-碘海醇复方脂质体的制备及包封率测定 1＊ 2 2 杨硕晔 ，王杏林 ，杨志强 （1.河南工业大学生物工程学院，郑州 475001；2.天津药物研究院，天津 300193） 中图分类号 R944 文献标志码 A 文章编号 1001-0408（2014）01-0048-04 DOI 10.6039/j.issn. 1001-0408.2014.01.17 摘 要 目的：制备洛莫司汀-碘海醇复方脂质体，并考察其质量、测定其包封率。方法：以逆相蒸发法制备复方脂质体；以磷脂种 类（A ）、磷脂与胆固醇质量比（B ）、脂质质量浓度（C ）为因素，以两主药的包封率为评价指标，采用正交设计法优化处方；以两主药 的包封率及脂质体的粒径和Zeta 电位为指标进行验证试验。结果：优化处方结果显示，A 为大豆磷脂80，B 为2∶1，C 为33 mg/ml。验证试验结果显示，洛莫司汀包封率约为75.7％，碘海醇包封率约为65.7％；脂质体粒径约为236.5nm ，Zeta 电位约为－42.2 mV 。结论：采用该处方与工艺可成功制备包封率较高的洛莫司汀-碘海醇复方脂质体，质量符合要求。 关键词 洛莫司汀；碘海醇；复方脂质体；制备；正交试验；包封率 Preparation of Lomustine-iohexol Compound Liposomes and Determination of the Entrapment Efficiency 1 2 2 YANG Shuo-ye ，WANG Xing-lin ，YANG Zhi-qiang （1.College of Bioengineering ，Henan University of Technol- ogy ，Zhengzhou 475001，China ；2.Tianjin Institute of Pharmaceutical Research ，Tianjin 300193，China ） ABSTRACT OBJECTIVE ：To prepare Lomustine-iohexol compound liposomes ，and to evaluate the properties and determine the entrapment efficiency. METHODS ：Compound liposomes were prepared by reverse evaporation method ；orthogonal design was used to optimize the formulation with the types of phospholipid （A ），the proportion of phospholipid to cholesterol （B ）and the con- tent of lipid （C ）as factors using the entrapment efficiency of two main components as index. The entrapment efficiency of two main components ，particle size and Zeta-potential of Compound lipidsomes were determined to validate the formulation. RE- SULTS ：The optimal formulation was as follows ：A was soybean phospholipid 80；B was 2∶1；C was 33 mg/ml. The entrapment efficiency of lomustine was 75.7％and that of iohexol was 65.7％；the particle size of compound liposomes was 236.5nm ，and Ze- ta potentials of them were －42.2mV. CONCLUSIONS ：The formulation and preparation technology can be used to prepare Lomus- tine-iohexol comp