N,N′-二甲基甲酰胺(DMF)桥联-β-环糊精/尼莫地平超分子配合物的制备及表征  

Preparation of N,N′-dimethyl formamide bridging-beta-cyclodextrin/nimodipine supramolecular complex and its characterization

作　　者：杨月琴[1] 杨润萍[1] 

机构地区：[1]大理学院附属医院药剂科,云南大理671000

出　　处：《现代医药卫生》2012年第24期3691-3693,共3页Journal of Modern Medicine & Health

摘　　要：目的通过利用尼莫地平与桥联环糊精形成超分子配合物,以进一步提高尼莫地平的水溶性及稳定性。方法查阅文献及相关资料,通过实验合成N,N′-二甲基甲酰胺(DMF)桥联-β-环糊精(简称桥联环糊精1),并对尼莫地平进行包合,用荧光光谱、一维核磁和红外光谱技术对尼莫地平和桥联环糊精1的超分子配合物在水溶液和固体状态中的包合行为进行考察和表征。结果桥联环糊精1与尼莫地平形成包合物后,尼莫地平的溶解度显著增加。桥联环糊精1可增加尼莫地平的溶解度、每毫克从1.88×10-3mol/L增加到4.62×10-6mol/L,由于主客体分子之间采用的协同键合模式,相比较天然环糊精,桥联环糊精1对尼莫地平给出了较高的键合常数。结论包合物使尼莫地平的稳定常数和水溶性均得到极大提高。Objective To prepare the supramolecular complex by using nimodipine and bridging-beta-cyclodextrin to further increase the water-solubility and stabilty of nimodipine.Methods Refering to the literature and relative data,N,N′-dimethyl formamide（DMF） bridging-beta-cyclodextrin（bridging cyclodextrin 1）was synthetized by experiment.Nimodopine was conducted the inclusion.The fluorescence spectroscopy,one dimensional nuclear magnetic resonance and infrared spectrum techniques were adopted to investigate and characterize the inclusion behaviour of supramolecular compound of nimodipine and bridging cyclodextrin 1 in aqueous solution and solid status.Results After the formation of inclusion compound of bridging cyclodextrin 1 and nimodipine,the solubility of nimodipine was significantly increased.Bridging cyclodextrin 1 could increase the nimodipine solubility from 1.88×10^-6 mol/L to 4.62×10^-3 mol/L per mg.Because adopting the collaborative bond model between the subject and object molecules,compared to natural cyclodextrins,bridging cyclodextrin 1 gave higher bond constant to nimopdipine.Conclusion Inclusion compound extremely increases the stability constant and water-solubility of nimodipine.

关 键 词：二甲基甲酰胺 β环糊精类 尼莫地平 光谱分析 药物稳定性 包合物 超分子化学 

分 类 号：R972.4[医药卫生—药品]