恩替卡韦分散片的制备及质量控制  

Preparation and quality control of entecavir dispersible tablets

作　　者：李冬梅[1,2] 吴燕[2] 石晟怡[3] 张福成[2] 

机构地区：[1]河北北方学院,张家口075000 [2]空军总医院,北京100142 [3]沈阳药科大学,沈阳110016

出　　处：《中国新药杂志》2013年第18期2179-2185,共7页Chinese Journal of New Drugs

摘　　要：目的:制备恩替卡韦分散片,并建立其质量控制方法。方法:以乳糖、微晶纤维素、交联聚维酮、聚维酮等压制恩替卡韦分散片;采用HPLC法分别检测分散片的含量、有关物质及对映异构体,其中以梯度洗脱方法分离恩替卡韦的B,C,D,E 4种已知杂质及其他未知杂质,以手性色谱柱分离其对映异构体。结果:确定了恩替卡韦分散片的处方组成,有关物质杂质可以得到有效分离。结论:本实验制得的恩替卡韦分散片处方合理,工艺简单;分析方法可以快速分离恩替卡韦的4种已知杂质和1种对映异构体,有效控制制剂中恩替卡韦杂质的限度。Objective ： To prepare entecavir dispersible tablets, and to establish a method of quatity control for the dispersible tablets. Methods： Entecavir dispersible tablets were made of lactose, MCC101, PVPK, PVPK30 and others. HPLC method was used to detect drug content, the related substances and its optical isomer. Gradient elution was adopted to separate four kinds of known impurities and other unknown impurities. Enantiomer was separated by chiral column. Results： The composition of the prescription of entecavir dispersible tablets was determined. Entecavir and impurities could be effectively separated. Conclusion： The formula and preparation process of entecavir dispersible tablets are reasonable and simple. Four impurities and one optical isomer can be quickly separated from entecavir by HPLC method, and the impuritiy limits can be effectively controlled.

关 键 词：恩替卡韦分散片 有关物质 对映异构体 梯度洗脱 

分 类 号：R978.7[医药卫生—药品] R943[医药卫生—药学]