以4,4'-联吡啶为配体的木犀草素药物共晶的合成及表征  

Synthesis and characterization of Pharmaceutical Co-crystal of Luteolin with 4, 4'-Dipyridy

作　　者：张羽男[1,2] 殷和美 张宇[2] 赵巍[2] 刘立新[2] 张大俊[2] 匡海学[1] 

机构地区：[1]黑龙江中医药大学,哈尔滨150040 [2]黑龙江省药学研究所,佳木斯大学,黑龙江佳木斯154007

出　　处：《东北农业大学学报》2015年第12期72-78,共7页Journal of Northeast Agricultural University

基　　金：中国博士后科学基金资助项目(2014M561382);佳木斯大学研究生科技创新项目(LM2015_094);佳木斯大学创新团队项目(CXTD-2013-05)

摘　　要：利用溶液挥发法首次合成1个全新的木犀草素-4,4'-联吡啶药物共晶,并通过红外光谱、核磁共振、X射线粉末衍射及差示扫描热量分析等对其表征。选择不同物质量比的木犀草素与4,4'-联吡啶及不同反应溶剂为主要影响因素,探索并确定相应合成条件:木犀草素和4,4'-联吡啶以13的物质量比混合后溶于7.0 m L丙酮溶剂,25℃下搅拌3 h后,于室温下挥发,5 d后得到黄褐色粉末状晶体。结果表明,在极性相对较小的溶剂体系中,反应物分子间形成数目合适且方向饱和的氢键连接,可有效促进药物共晶生成。A new pharmaceutical co-crystal of Luteolin with 4, 4＇-dipyridy was firstly synthesized by solution evaporation method. The powder of luteolin-4, 4＇-dipyridy had been characterized by IR, NMR, XRD and DSC. By selecting different molar ratios of Luteolin and 4, 4＇-dipyridy and different reaction solvents as the main factors, the preparation condition was to be explored and to be obtained. Luteolin and 4, 4＇- bipyridy were combined in 7.0 mL acetone with stirring at 25 ℃ for 3 h, and their molar ration was 1：3. The resulting solution was filtered and allowed to evaporate slowly at room temperature. Then tan powdery crystals were obtained after 5 days. As results, it showed that hydrogen bonds with proper numbers and saturated direction between molecular could promote the formation of pharmaceutical co-crystals in solovent with weak polarity.

关 键 词：木犀草素 4 4’-联吡啶 药物共晶 溶液挥发法 

分 类 号：R194[医药卫生—卫生事业管理]