盐酸阿替卡因的多晶型研究  

Study on the polymorphs of articaine hydrochloride

作　　者：张国宏[1] 段亚波[1] 李翼[1] 吴松[1] 

机构地区：[1]中国医学科学院中国协和医科大学药物研究所,北京100050

出　　处：《中国新药杂志》2004年第9期813-816,共4页Chinese Journal of New Drugs

摘　　要：目的：建立盐酸阿替卡因多晶型的测定方法并研究其理化性质。方法：研究了不同晶型的盐酸阿替卡因的制备方法，采用熔点测定、差示扫描量热法(DSC)、红外吸收光谱法(IR)及粉末X-衍射法(Powder X-ray)研究了不同晶型的特征，并考察了2种晶型在高湿、高温和光照条件下的稳定性。结果：盐酸阿替卡因存在2种不同的晶型，晶型Ⅰ和晶型Ⅱ。通过熔点测定、DSC和IR分析及粉末X-衍射法可区分2种晶型。晶型Ⅰ有较强的吸湿性，而晶型Ⅱ不易吸湿，2种晶型对光照和高温均较稳定。结论：盐酸阿替卡的晶型Ⅱ适合作为药物应用。Objective:To establish methods for the detection of physical and chemical characteristics of the polymorphs of articaine hydrochloride crystals. Methods: Two polymorphic forms of arti caine hydrochloride crystals were obtained. The polymorphs of articaine hydrochloride crystals were determined by melting point,differential scanning calorimetry (DSC), IR spectra (IR) and powder X-ray diffraction. The stability of the two polymorphs was measured under heat,light and humidity. Results: Two polymorphs of articaine hydrochloride crystals were defined as form Ⅰ and form Ⅱ. The two polymorphic forms showed different melting points, DSC, IR,and powder X-ray diffraction patterns. The form Ⅰ had higher hygroscopicity than the form Ⅱ. Conclusion: Form Ⅱ is more stable form a gainst humidity,and suitable to be a drug substance.

关 键 词：盐酸阿替卡因 多晶型 药物应用 研究 IR 粉末 X-衍射 熔点测定 DSC 制备方法 

分 类 号：R914[医药卫生—药物化学] TQ325[医药卫生—药学]