β-环糊精高聚物-高乌甲素包合物的制备、表征及增溶性

发布时间：2018-04-21 00:00

本文选题：高乌甲素 + β-CD高聚物　；参考：《中国新药杂志》2015年01期

【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。
[Abstract]:Aim: to prepare and investigate the inclusion complex of lamella- 尾 -CDPH and its related properties. Methods: three kinds of inclusion complexes of 尾 -CD, 尾 -CD oligomer (尾 -CDPLN, 尾 -CDPHand) with aconitine were prepared by saturated ethanol aqueous solution method. The inclusion complexes were identified by UV, IR and DSC. The contents and solubility of the three inclusion complexes were investigated by UV spectrophotometry, and the release of LA- 尾 -CDPH inclusion compounds in vitro was determined by simulating the pH values of human stomach, intestine and blood. Results: 尾 -CDPH and LA formed inclusion complexes with a molar ratio of 1:1. The average content of LA in the inclusion complexes was 27 卤1.1, and the solubilization of LA was 11 978 mg / L, 3.9 times as much as that of LA- 尾 -CD inclusion complexes and 1.5 times as much as that of LA- 尾 -CDPL inclusion complexes. In vitro release test showed that the release time could reach 8 hours in simulated blood environment. Conclusion the preparation process of the inclusion compound of 尾 -CDPH is simple, the solubility of the drug is improved significantly, and the LA drug has a certain slow-release effect in simulated human blood environment.
【作者单位】：内蒙古农业大学食品科学与工程学院;
【基金】：内蒙古自然科学基金(2011BS1203)
【分类号】：TQ460.1;R943

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