【摘要】 利用盐酸川芎嗪(Lig-HCl)分别与安赛蜜钾(Ace-K)和糖精钠(Sac-Na)进行离子交换制得2种川芎嗪新盐安赛蜜川芎嗪(Lig-Ace)和糖精川芎嗪一水合物(Lig-Sac),并通过X射线衍射(XRD)、红外光谱扫描(IR)、热失重分析(TG)、差示扫描量热分析(DSC)对其进行结构表征和热分析;以磷酸川芎嗪(TMPP)作为参比,测定2种新盐的溶解度和体外粉末溶出,口服顺应性(口感)以及升华特性。XRD和IR结构表征显示成功制备出Lig-Ace和Lig-Sac 2种川芎嗪新盐,其中Lig-Sac热不稳定,易分解,Lig-Ace相对较稳定,熔点为227℃;Lig-Ace的稳定性相对较好,不易升华。Lig-Ace比Lig-Sac的溶解度高,TMPP溶解度处于两者之间,而2种新盐的口感均为甜的。结果表明,通过离子交换法制得了适用于口服的2种稳定的甜的川芎嗪新盐,丰富了川芎嗪临床用药的选择性。更多还原

【Abstract】 In this study,two kinds of sweet ligustrazine salts were prepared by anion exchange reaction with acesulfame potassium(Ace-K) and sodium saccharin(Sac-Na) respectively using ligustrazine hydrochloride(Lig-HCl):acesulfame ligustrazine(Lig-Ace) and saccharin ligustrazine monohydrate(Lig-Sac).X-ray diffraction(XRD),infrared spectroscopy(IR),thermogravimetric analysis(TG),differential scanning calorimetry(DSC) were used for structural characterization and thermal analysis.Compared with the properties of tetramethylpyrazine phosphate(TMPP),the solubility and powder dissolution,oral compliance(mouthfeel),sublimation properties of the two new salts were determined to investigate the differences between the two new salts and ligustrazine phosphate.XRD and IR structural characterization showed that two new ligustrazine salts,Lig-Ace and Lig-Sac,were successfully prepared.Lig-Sac is thermally unstable and easily decomposed.Lig-Ace is relatively stable and has a melting point of 227℃.Lig-Ace has relatively great stability and is not easy to sublimate.The solubility of TMPP is between Lig-Sac and Lig-Ace,but the oral compliance of the two new salts is significantly better than that of TMPP.The results showed that two new ligustrazine salts suitable for oral administration were prepared by ion exchange method,which enriched the selectivity of ligustrazine.更多还原