【摘要】 目的:应用2-羟丙基-β-环糊精(2-HP-β-CD)包合抗幽门螺杆菌新化学实体NE-2001,系统观察包合作用和计算热力学参数,确定达到最佳包合效果的制备方法。方法:通过正交实验选择NE-2001与2-HP-β-CD之间包合作用的最佳条件,采用冷冻干燥技术制备NE-2001-2-HP-β-CD包合物,经X-射线衍射(XRD)和差示扫描量热法(DSC)对后者进行鉴定,并与其他3种环糊精的包合效应进行比较。结果:包合的最优条件是主客分子物质的量比为5:1．温度为50℃,时间为45 min,此时达到本实验的最大增溶特性及结合常数。运用X-射线衍射和差示扫描量热法分析确证冻干粉末已经形成包合物。结论:经2-HP-β-CD包合后,NE-2001的溶解度获得显著提高。更多还原

【Abstract】 Objective:To optimize the preparation of an inclusion complex of NE-2001 , a new chemical entity against Helicobacter pylori, using 2-hydroxypropyl-β-eyclodextrin (2-HP-β-CD). Methods:The process for the inclusion complex of NE-2001 with 2-HP-β-CD were optimized using an orthogonal test; the target inclusion complex was prepared by a lyophilizing technique. The quality of the inclusion complex was determined by X-ray diffraction ( XRD) and differential scanning calorimetry ( DSC) as well as comparison with other three types of cyclodextrins. Results:The optimal parameters of the process for the inclusion complex included a molar ratio of 2-HP-β-CD to NE-2001 5: 1 , reaction temperature at 50℃and inclusion period for 45 min. Under these conditions, the inclusion complex had maximal values of solubility and reaction constant KC, XRD and DSC analyses confirmed that the lyophilizing powder had features of an inclusion complex. Conclusion:The solubility of NE-2001 was significantly improved as a result of the inclusion complex with 2-HP-β-CD.更多还原