青藤碱- 环糊精包合工艺的优化及包合常数测定

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。

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

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.