青藤碱-环糊精包合工艺的优化及包合常数测定  

Optimization of Preparation Process for Sinomenine-Cylcodextrin Inclusion Complex and Its Inclusion Constant

作　　者：朱士龙[1] 李勇[1] 林红卫[2,3] 段友构[1] 

机构地区：[1]吉首大学化学化工学院,湖南吉首416000 [2]怀化学院化学化工系,湖南怀化418008 [3]民族药用植物资源研究与利用湖南省重点实验室,湖南怀化418008

出　　处：《食品科学》2012年第8期54-59,共6页Food Science

基　　金：国家自然科学基金面上项目(30870230);湖南省自然科学基金项目(06JJ50020);湖南省教育厅项目(09C760);民族药用植物资源研究与利用湖南省重点实验室开放基金项目(HHUW2010-68);吉首大学研究生校级科研项目(11JDY052)

摘　　要：目的:考察青藤碱与环糊精形成包合物的最佳条件,测定青藤碱与不同环糊精的包合常数并进行体外释放研究。方法:通过单因素及正交试验确定青藤碱与不同环糊精形成包合物的最佳条件,并在此条件下利用相溶解度法测定青藤碱与β-环糊精、羟丙基-β-环糊精、γ-环糊精的包合常数,对包合物进行体外释放试验研究。结果:青藤碱与不同环糊精形成包合物的最佳条件为物质的量的1:1、包合温度50℃、包合反应3h、包合反应时溶液pH7,青藤碱与β-环糊精、羟丙基-β-环糊精、γ-环糊精的包合常数分别为501.1、150.0、600.3L/mol。结论:青藤碱与环糊精可以形成1:1型稳定的包合物,以环糊精为载体制备的不同青藤碱-环糊精包合物相对于青藤碱具有明显的缓释作用。Objectives： To investigate optimal conditions for inclusion complex formation between sinomenine and cylcodextrins and determine the inclusion constants and release in vitro of inclusion complexes prepared with different cyclodextrins.Methods： One-factor-at-a-time and orthogonal array design methods were employed for the optimization of inclusion complex formation conditions.The inclusion constants of sinomenine complexes with β-cylcodextrin（β-CD）,hydroxypropyl-β-cyclodextrin（HP-β-CD） and γ-cyclodextrin（γ-CD） formed under optimal conditions were determined by the phase solubility method.Moreover,their release in vitro was tested.Results： The optimal conditions for forming sinomenine-cylcodextrins inclusion complexes were 1：1 of sinomenine-to-cylcodextrin molar ratio,50 ℃ of temperature,and 3 h of reaction duration at pH 7.The inclusion constants of sinomenine-β-CD,sinomenine-HP-β-CD and sinomenine-γ-CD formed under these conditions were calculated as 501.1,150.0,600.3 L/mol,respectively.Conclusion： sinomenine and cylcodextrins can form stable inclusion complexes at a molar ratio of 1：1.Various inclusion complexes show remarkable sustained release effect on sinomenine.

关 键 词：青藤碱 环糊精 包合常数 正交试验设计 工艺优化 

分 类 号：TQ460.4[化学工程—制药化工]