β-环糊精高聚物-高乌甲素包合物的制备、表征及增溶性  

Preparation,identification and solubilization of β-cyclodextrin polymer-lappaconitine inclusion compound

作　　者：王雪娇[1] 董同力嘎 张师[1] 王红[1] 苏美玲[1] 靳烨[1] 孙文秀[1] 

机构地区：[1]内蒙古农业大学食品科学与工程学院,呼和浩特010018

出　　处：《中国新药杂志》2015年第1期102-106,共5页Chinese Journal of New Drugs

基　　金：内蒙古自然科学基金(2011BS1203)

摘　　要：目的:制备高乌甲素-β-CD高聚物包合物(LA-β-CDPH包合物),并考察包合物相关性质。方法:采用饱和乙醇水溶液法制备了β-CD、β-CD低聚物(β-CDPL)、β-CD高聚物(β-CDPH)与高乌甲素所形成的3种包合物,采用紫外光谱、红外光谱以及差示量热扫描法对包合物进行鉴定,通过紫外光谱法考察3种包合物中药物含量、溶解度,同时模拟人体胃、肠及血液p H值环境对LA-β-CDPH包合物进行体外释放测试。结果:β-CDPH与LA能形成摩尔比为1∶1的包合物,包合物中LA平均含量可达(27±1.1)%,且对LA增溶量可达11 978 mg·L-1,分别是LA-β-CD包合物增溶量的3.9倍、LA-β-CDPL包合物增溶量的1.5倍,体外释放实验表明在模拟血液环境下释放时间可达8 h。结论:LA-β-CDPH包合物制备工艺简单,且显著提高了药物的溶解性,并使LA药物在模拟人体血液环境下有一定的缓释效果。Objective： To prepare the inclusion compound of lappaconitine-β-CDPH （LA-β-CDPH） and investigate its properties. Methods： The inclusion compounds of LA-β-CD, LA-[3-CDPL and LA-β-CDPH were prepared by a saturated aqueous solution method, and identified by UV-vis spectroscopy, FT-IR and DSC. The content of lappaconitine in the inclusion complex and the solubility of three kinds of inclusion compound were investigated by a UV spectrophotometer method. The physiological parameters of stomach, small intestine and blood pH value were simulated to investigate the in vitro release. Results： The inclusion compounds were obtained, and the molecular ratio of lappaconitine to β-CDPH was 11 ： 11 with a mean drug content of （27 ± 1. 1 ） %. Compared to β-CD and β-CDPL, the solubility increased by 1.5 and 3.9 times after lappaconitine was included with β-CDP, arriving at 11 978 mg·L-1 After inclusion, a sustained release of lappaconitine from lappaconitine-β-CDP, was observed, achieving 8 h. The water solubility was significantly improved. Conclusion： The technique of preparing lappaconitine-β-CDP inclusion compound is simple, and the inclusion compound can increase solubility and has a sustained release property.

关 键 词：高乌甲素 β-CD高聚物 包合物 溶解性 体外释放 

分 类 号：R943.4[医药卫生—药剂学]