15个厂家布洛芬缓释胶囊仿制药与参比制剂溶出曲线的比较  

Comparison of dissolution profile of ibuprofen sustained-release capsules between 15 manufacturers'generics and reference formulations

作　　者：李志芳[1] 丁怡[1] 冯金元[1] 石颖 章娟[1] LI Zhi-fang;DING Yi;FENG Jin-yuan(Guangzhou Institute for Drug Control,Guangzhou 510160,China)

机构地区：[1]广州市药品检验所,广州510160

出　　处：《中国处方药》2024年第5期30-33,共4页Journal of China Prescription Drug

基　　金：广州市市场监督管理局科技项目(2022kj35);广东省药品监督管理局科技创新项目(2020ZDB06)。

摘　　要：目的通过比较15个厂家生产的布洛芬缓释胶囊与参比制剂的体外溶出曲线,为其质量一致性评价提供参考。方法以pH1.0盐酸溶液、pH4.0醋酸盐缓冲液、pH6.0磷酸盐缓冲液和pH7.2磷酸盐缓冲液分别作为溶出介质,体积为900 ml,采用篮法,转速为30 r/min,进行释放度考察,采用高效液相色谱(HPLC)法测定布洛芬的含量,并计算累积溶出量,绘制溶出曲线,采用差异因子(f_(1))和相似因子(f_(2))法评价溶出曲线的相似性。结果厂家A在pH1.0盐酸溶液和pH4.0醋酸盐缓冲液介质中,与参比制剂相比,f_(1)>15,溶出曲线有差异。其他14个厂家与参比制剂在4种溶出介质中,f_(1)均<15且f_(2)均>50,溶出曲线相似,溶出行为一致。结论厂家A仿制制剂与原研地产化参比制剂在非药典溶出度检查项目规定的溶出介质中存在溶出行为不完全一致的情况,可能与其处方及生产工艺有关,仍需结合具体的生物等效性试验以及其他药学指标进行一致性的全面评估。Objective To compare the in vitro dissolution profiles of ibuprofen sustained-release capsules between 15 manufacturers'generic and reference formulations,in order to provide reference for the evaluation of quality consistency.Methods The dissolution medium used in this study were pH 1.0 hydrochloric acid solution,pH 4.0 acetate buffer,pH 6.0 phosphate buffer and pH 7.2 phosphate buffer,respectively,with the volume of 900 ml.The basket method was applied at the rotation speed of 30 r/min.The content of ibuprofen was determined by HPLC.The cumulative dissolution was calculated and the dissolution curves were obtained.The difference factor(f_(1))and similarity factor(f_(2))method were used to evaluate the similarity of dissolution profiles.Results Among the domestic generic preparations,products from manufacturer A in pH 1.0 hydrochloric acid solution or pH 4.0 acetate buffer,the f_(1) were more than 15,which were not similar to the reference formulations,there were differences in the dissolution curves.Products from the other 14 manufacturers,in the four dissolution media,all f_(1) were less than 15 and all f_(2) were more than 50,the dissolution profiles were similar and the dissolution behaviors were consistent to the reference formulations.Conclusion In the dissolution medium not specified in the pharmacopoeia of ibuprofen sustained-release capsules,generic preparations from manufacturer A have dissimilar dissolution profiles and inconsistent dissolution behaviors,which may be related to its prescription and production technology.In order to make a comprehensive assessment of the consistency of ibuprofen sustained-release capsules,the specific bioequivalence experiments and other indicators of pharmacy still needs to be integrated for the reference and domestic generic preparations from different sources.

关 键 词：布洛芬缓释胶囊 释放度 溶出曲线 差异因子 相似因子 

分 类 号：R927.1[医药卫生—药学]