外用半固体制剂质量研究与体外评价技术进展  

Progress in applications of quality research and in vitro evaluation technology in topical semi-solid preparations

作　　者：罗婷婷 庾莉菊[1] 宁保明[1] 孙春萌[2] 涂家生[2] 梁晓静 LUO Ting-ting;YU Li-ju;NING Bao-ming;SUN Chun-meng;TU Jia-sheng;LIANG Xiao-jing(National Institutes for Food and Drug Control,Key Laboratory of National Medical Products Administration-Key Laboratory of Research and Evaluation of Chemical Drug Quality,Beijing 102629,China;China Pharmaceutical University,Nanjing 210019,China;Logan Instruments Corp.,New Jersey 08873,USA)

机构地区：[1]中国食品药品检定研究院,国家药品监督管理局重点实验室-化学药品质量研究与评价重点实验室,北京102629 [2]中国药科大学药学院,南京210019 [3]Logan公司,美国新泽西州08873

出　　处：《药物分析杂志》2022年第5期748-760,共13页Chinese Journal of Pharmaceutical Analysis

基　　金：国家药典委员会2022年标准提高课题——0931溶出度与释放度测定法扩散池法的建立(2022Y03)。

摘　　要：外用半固体制剂用途广泛,但处方、制剂特性复杂,工艺参数控制难度高,微小的处方工艺变化都可能导致产品质量的显著差异,其与吸入制剂、透皮贴剂等都属于研发难度大,在审评过程中需要根据具体品种个性化考虑的复杂制剂。能区分不同处方和工艺,且具有体内外相关性的体外评价研究,可以更好地满足外用半固体制剂的质量研究和审评技术要求。本文以复杂制剂的研究为重点,在查阅国内外相关的文献报道和政策法规的基础上,参考国内外监管机构对外用半固体制剂的评价要求和品种指南(product-specific guidances,PSGs),结合自身研究工作的发现和思考,综述了外用半固体制剂的应用、政策法规以及质量控制等方面的现状,着重对如何建立科学的外用半固体制剂的体外评价体系进行了探讨,初步分析了外用半固体制剂建立体内外相关性的技术难点,期望为外用半固体仿制药开发及产品变更研究提供借鉴。Topical semi-solid preparations are widely used,however,the formulation and preparation characteristics are complex,and the process parameters are difficult to control.Small changes in the formulation and manufacturing process may cause significant differences in product quality.Topical semi-solid preparations,inhalation preparations and transdermal patches are complex preparations that are difficult to develop and need to be considered individually according to specific varieties during the R&D and review process.In vitro evaluation studies that can distinguish different prescriptions and processes and have in vitro and in vivo correlation can better meet the technical requirements of quality research and evaluation of topical semi-solid preparations.This paperfocuses on the research of complex preparations,based of consulting relevant literature,policies and regulations,referring to the evaluation requirements and product-specific guidance of domestic and foreign regulatory agencies for topical semi-solid preparations,combined with the findings and thinking of the author’s own research work.This review gives the current application,policies and regulations and quality control of topical semi-solid preparations,further focuses on how to establish a scientific in vitro evaluation system for topical semi-solid preparations,and preliminarily analyzes technical difficulties in establishing in vivo and in vitro correlations.It is expected to provide reference for the development and product changes research of topical semi-solid generic drugs.

关 键 词：复杂制剂 外用半固体制剂 经皮给药 体外释放 体外渗透 体外透皮吸收 流通池 扩散池 浸没池 体内外相关性 

分 类 号：R917[医药卫生—药物分析学]