咪唑斯汀缓释片仿制药与原研药质量对比研究  

Comparative Study on the Quality of Mizolastine Sustained-Release Tablets Generic and Original-Patented Drugs

作　　者：崔亚宁 邓颖鹏 张思楠 雷轩 CUI Yaning;DENG Yingpeng;ZHANG Sinan;LEI Xuan(Shaanxi Institute for Food and Drug Control,Xi′an,Shaanxi,China 710065;National Medical Products Administration Key Laboratory of Drug Microbiological Testing Technology,Xi′an,Shaanxi,China 710065;Shaanxi University of Chinese Medicine,Xianyang,Shaanxi,China 712046)

机构地区：[1]陕西省食品药品检验研究院,陕西西安710065 [2]国家药品监督管理局药品微生物检测技术重点实验室,陕西西安710065 [3]陕西中医药大学,陕西咸阳712046

出　　处：《中国药业》2023年第10期76-80,共5页China Pharmaceuticals

基　　金：陕西省药品监督管理局科学监管与监管科学研究项目[SXYJ202106]。

摘　　要：目的比较咪唑斯汀缓释片仿制药与原研药的质量。方法采用紫外-可见分光光度法测定制剂中咪唑斯汀的含量;以0.1 mol/L盐酸、0.01 mol/L盐酸、醋酸盐缓冲液(pH 3.8)及醋酸盐缓冲液(pH 4.5)为溶出介质,测定溶出度,并绘制溶出曲线;采用高效液相色谱法测定仿制药和原研药中有关物质含量。结果咪唑斯汀缓释片仿制药和原研药咪唑斯汀含量分别为标示量的98.19%~102.80%和100.70%~101.35%,相对偏差(RD)分别为0.29%~0.56%和0.21%~0.29%;两者在4种溶出介质中的溶出曲线差异较大,无法采用相似因子法对相关溶出度进行相似度评价;3批次仿制药中有关物质Ⅰ总量均为0.25%,有关物质Ⅱ总量分别为0.57%,0.54%,0.57%,3批次原研药中上述有关物质总量分别小于0.05%和0.10%。结论咪唑斯汀缓释片仿制药与原研药质量存在一定差异。建议有关厂家从制剂原料药及辅料、制备工艺等方面进行优化,提升仿制药质量,为仿制药一致性评价工作提供支撑。Objective To compare the quality of Mizolastine Sustained-Release Tablets generic and original-patented drugs.Methods The content of mizolastine in the preparation was determined by the ultraviolet-visible spectrophotometry method.The dissolution was determined and the the dissolution profile was drawn with the hydrochloric acid(0.1 mol/L),hydrochloric acid(0.01 mol/L),acetate buffer(pH 3.8)and acetate buffer(pH 4.5)as the dissolution media.The contents of related substances in the generic and original-patented drugs were determined by the high-performance liquid chromatography(HPLC)method.Results The contents of mizolastine in the Mizolastine Sustained-Release Tablets generic and original-patented drugs were in the range of 98.19%-102.80%of labelled amount and 100.70%-101.35%of labelled amount respectively,and the relative deviations(RDs)were in the range of 0.29%-0.56%and 0.21%-0.29%respectively.The dissolution profiles of Mizolastine Sustained-Release Tablets generic drug differed significantly from those of original-patented drug in the above four dissolution media,making it impossible to use the similarity factor method to evaluate the similarity of related dissolution.The total content of related substanceⅠin the three batches of generic drugs was 0.25%,while the total content of related substanceⅡin the above generic drugs was 0.57%,0.54%and 0.57%respectively.The total contents of related substanceⅠand related substanceⅡin the three batches of original-patented drugs were less than 0.05%and 0.10%respectively.Conclusion The quality of Mizolastine Sustained-Release Tablets generic drug is different from that of the original-patented drug.It is suggested that relevant manufacturers should make corresponding optimizations in the aspects of raw materials,excipients,preparation processes and so on to improve the quality of generic drug and provide a favorable support for its consistency evaluation.

关 键 词：咪唑斯汀缓释片 紫外-可见分光光度法 高效液相色谱法 一致性评价 

分 类 号：R917[医药卫生—药物分析学] R927[医药卫生—药学]