长春瑞滨磷脂复合物的制备及其性质研究  

Preparation of vinorelbine-phospholipid complex and its characterization

作　　者：李艳贞[1] 阎卉[1] 刘欢[1] 靳文仙[1] 王成港[1] 

机构地区：[1]天津药物研究院释药技术与药代动力学国家重点实验室,天津300193

出　　处：《现代药物与临床》2012年第6期570-574,共5页Drugs & Clinic

基　　金：国家重点基础研究发展计划(973计划)课题(2010CB735602;2012CB724002);国家重大新药创制科技重大专项--国家生物医药国际创新园(天津)创新药物孵化基地建设(2010ZX09401)

摘　　要：目的制备长春瑞滨磷脂复合物,提高药物的脂溶性,以期进一步制备长春瑞滨微粒载药系统。方法采用溶剂挥发法制备长春瑞滨磷脂复合物,以复合率为评价指标进行单因素优化试验。采用差示扫描量热法、X射线衍射法、紫外分光光度法对复合物进行鉴别,并考察复合物的体外溶解性质变化。结果优化条件下制备的磷脂复合物复合率为89.3%～93.7%;差示扫描量热法、X射线衍射法、紫外分光光度法验证了复合物的形成;形成磷脂复合物后,长春瑞滨的脂溶性显著提高。结论制备的长春瑞滨磷脂复合物能显著增加药物的脂溶性,为进一步制备长春瑞滨微粒载药系统奠定基础。Objective To prepare vinorelbine-phospholipid complex （VPC） for enhancing the liposolubility of vinorelbine.MethodsThe complex was prepared using solvent evaporation method.The preparation technology was optimized by single factor design,usingthe combining ratio as the assessment index.Differential scanning calorimetry （DSC）,X-ray diffraction （XRD） spectrum,and UVspectrophotometry were carried out to investigate its characterization.The in vitro solubility change of the complex was alsodetermined.Results The combining ratio of the complex prepared under the optimized conditions was between 89.3% and 93.7%;UV spectrum,DSC and XRD spectra confirmed the formation of the complex.After phospholipid complex being made,theliposolubility of vinorelbine was remarkably enhanced.Conclusions Prepared vinorelbine-phospholipid complex could effectivelyenhance the liposolubility of vinorelbine and provide the reference for preparation of vinorelbine microsomal drug-loaded system.

关 键 词：长春瑞滨磷脂复合物 长春瑞滨 复合率 差示扫描量热法 X射线衍射法 紫外分光光度法 

分 类 号：R944.2[医药卫生—药剂学]