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β-环糊精高聚物-高乌甲素包合物的制备、表征及增溶性 被引量:3

Preparation,identification and solubilization of β-cyclodextrin polymer-lappaconitine inclusion compound
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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.
出处 《中国新药杂志》 CAS CSCD 北大核心 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)
关键词 高乌甲素 β-CD高聚物 包合物 溶解性 体外释放 lappaconitine β-CDP inclusion compound solubility in vitro release
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