穿心莲内酯-羟丙基-β-环糊精包合物的鉴定和热力学稳定性研究  

Identification of andrographolide hydroxypropyl-β-cyciodextrin inclusion compound and study on its thermodynamic stability

作　　者：任科[1] 张志荣[1] 鞠静红[1] 刘阳[1] 龚涛[1] 

机构地区：[1]四川大学华西药学院靶向药物及传递系统教育部重点实验室,四川成都610041

出　　处：《中草药》2008年第4期518-521,共4页Chinese Traditional and Herbal Drugs

摘　　要：目的制备和鉴定穿心莲内酯-羟丙基-β-环糊精包合物,并考察穿心莲内酯和羟丙基-β-环糊精之间的包合摩尔比及包合过程的热力学常数。方法采用冷冻干燥法制备穿心莲内酯-羟丙基-β-环糊精包合物,采用差示扫描量热法(DSC)、X射线衍射(XRD)和红外光谱法(IR)对包合物进行鉴定,通过表观溶解度法考察包合物中主客分子之间的包合摩尔比及包合过程的热力学常数。结果25、35、45 C下穿心莲内酯和羟丙基-β-环糊精能形成1:1摩尔比包合物.相溶解度图呈A_L型,包合过程为放热反应。结论穿心莲内酯-羟丙基-β-环糊精包合物能显著增大药物的溶解度。Objective To prepare and identify the andrographolide-hydroxypropyl-β-cyclodextrin （andrographolide-HP-β-CD） inclusion compound. The mol ratio between andrographolide and HP-β-CD and the thermodynamic constants in inclusion were studied simultaneously. Methods The andrographolide-HP-β-CD inclusion compound was prepared with lyophilization technique. Meanwhile, the inclusion compound was identified by differential scanning calorimetry （DSC） methods, infrared spectrometry （IR）, and X-ray diffraction （XRD）, respectively. The mol ratio between host and guest moleculars and the thermodynamic constants during the inclusion process were also researched by phase solubility method. Results An 1 ： 1 molar ratio inclusion complex of andrographolide with HP-β-CD could be formed at 25, 35, and 45℃. The phase diagram was AL type and the procedure of inclusion was a heat release process. Conclusion The solubility of andrographolide-HP-β-CD inclusion compound can be increased obviously by the above-mentioned preparing techniques.

关 键 词：穿心莲内酯 包合物 差示扫描量热法 红外光谱法 X射线衍射 相溶解度法 

分 类 号：R284.4[医药卫生—中药学] R286.02[医药卫生—中医学]