国产、进口及国外三种吗替麦考酚酯胶囊的体外溶出曲线对比研究

Comparative studies on dissolution profiles of three Mycophenolate Mofetil Capsules in different dissolution mediums

目的通过建立有区分力的溶出曲线测定方法,对国产、进口原研及美国橙皮书收载的参比制剂三种吗替麦考酚酯胶囊进行体外溶出曲线的对比研究,以评价国产制剂、进口及国外原研参比制剂溶出行为的一致性。方法参考美国FDA溶出曲线数据库、日本IF文件及中国药典公布的吗替麦考酚酯胶囊溶出检测条件,选择0.1 N HCl、水、pH6.8磷酸盐缓冲液和pH5.0柠檬酸缓冲液4种不同pH值的溶出介质,对国内外上市的三种吗替麦考酚酯胶囊溶出曲线进行对比研究,通过相似因子(f2)法对溶出曲线进行评价。结果三种制剂在0.1 N HCl介质中15 min累计溶出量均大于85%;国产制剂与国内外参比制剂在水、pH6.8磷酸盐缓冲液和pH5.0柠檬酸缓冲液三种溶出介质中的溶出曲线相似因子f2均大于50。结论国产制剂、进口及国外三种制剂在4种不同溶出介质中的溶出曲线均一致。

Objective To compare the dissolution profiles of three Mycophenolate Mofetil Capsules,including domestic generic preparation、imported brand name preparation and RLD listed in the Orange book,in 4 different mediums and evaluate the quality difference between them.Methods Refer to dissolution methods under Mycophenolate Mofetil Capsules monographs published on FDA"dissolution database"、"Japanese IF"and Chinese"Pharmacopoeia"2015 edition,four different pH mediums,including 0.1 N HCl,water,pH6.8 phosphate buffer and pH5.0 acetate buffer,were selected to compare the dissolution profiles of three preparations.The dissolution profiles were evaluated by f2 similarity factor.Results Three preparations were rapidly dissolved in 0.1 N HCl medium.Similarity factors f2 in water,pH6.8 and pH5.0 are all greater than 50.Conclusion The dissolution profiles of the three preparations in four different pH dissolution mediums are similar.