盐酸地芬尼多片溶出度测定一致性评价及体内外相关性的研究  

Consistency Evaluation of the Dissolution of Difenidol Hydrochloride Tablets and Study of in vivo-in vitro Correlation

作　　者：黄丽丽 朱荣 奉艳花 朱健萍 卢日刚 Huang Lili;Zhu Rong;Feng Yanhua;Zhu Jianping;Lu Rigang(Guangxi Institute for Food and Drug Control,Nanning 530021,China)

机构地区：[1]广西壮族自治区食品药品检验所,南宁530021

出　　处：《中国药师》2020年第11期2138-2141,共4页China Pharmacist

基　　金：广西科技计划(重点研发计划)项目(编号:桂科AB17292049、桂科AB18221125);十三五国家科技专项“重大新药创制”课题(编号:2017ZX09101001)。

摘　　要：目的:研究评价国产盐酸地芬尼多片与参比制剂的体外溶出一致性,并分析体内外相关性。方法:参照中国药典2015年版方法,分别测定3批国产制剂与参比制剂在4种不同溶出介质(pH 1.2盐酸溶液、pH 4.0醋酸盐溶液、pH 6.8磷酸盐溶液、水)中的溶出度,绘制溶出曲线,采用相似因子(f2)法分析国产制剂与参比制剂的溶出曲线相似性。借助Gastroplus^TM软件结合体外溶出试验结果,建立盐酸地芬尼多片体内外相关性模型。结果:国产仿制制剂在4种溶出介质中的溶出行为与参比制剂不一致,f2法不适用于盐酸地芬尼多片的体外溶出一致性分析。软件分析结果提示体外溶出曲线与软件模拟的体内行为不相似。结论:国产盐酸地芬尼多制剂质量有待提高,溶出一致性评价方法待进一步研究。Objective:To research the in vitro dissolution consistency between generic and original preparations of difenidol hydrochloride tablets,and to establish the in vivo-in vitro correlation.Methods:According to Chinese Pharmacopeia(2015 edition),the dissolutions of generic preparations with three batches and original preparation in 4 different dissolution media(pH 1.2 hydrochloric acid solution,pH 4.0 sodium acetate solution,pH 6.8 phosphate solution,water)were determined,and then the dissolution curves were drawn,and the similarity factors(f2)were calculated to evaluate the in vitro dissolution consistency between the generic and original preparations.The GastroPlus^TM software was used to analyze the in vivo-in vitro correlation.Results:The dissolution properties of generic preparations with three batches were different from those of original preparation in four media.Similarity factors were not suitable for the consistency evaluation of dissolution properties of difenidol hydrochloride tablets in vitro.The results of Gastro Plus^TManalysis indicated that the dissolution behavior of difenidol hydrochloride tablets in vitro and in vivo had no significant correlation.Conclusion:The quality of domestic difenidol hydrochloride tablets needs to be improved,and the evaluation method of dissolution consistency needs to be further studied.

关 键 词：盐酸地芬尼多片 溶出度 一致性评价 Gastro Plus^TM软件 

分 类 号：R917[医药卫生—药物分析学]