用于经皮给药系统研究的皮肤模型与关键质量控制  

Skin Models and Critical Quality Control for the Studies of Transdermal Drug Delivery Systems

作　　者：朱慧勇[1] 武余波[1] 卢望丁 杨晓钰 胡阳阳 罗华菲[1] ZHU Huiyong;WU Yubo;LU Wangding;YANG Xiaoyu;HU Yangyang;LUO Huafei(National Pharmaceutical Engineering Research Center,China State Institute of Pharmaceutical Industry,Shanghai 201203)

机构地区：[1]中国医药工业研究总院药物制剂国家工程研究中心,上海201203

出　　处：《中国医药工业杂志》2022年第5期592-600,共9页Chinese Journal of Pharmaceuticals

摘　　要：皮肤模型是经皮给药系统产品开发中必须涉及的材料,皮肤模型的屏障性能是研究药物经皮渗透的关键要素之一。氚水(HO)体外经皮渗透和经皮水分蒸发(TEWL)是评价皮肤屏障功能的有效方法和重要指标。本研究表明,将皮肤的新鲜度、厚度、质量、TEWL达到稳态等因素作为皮肤模型的质量控制手段,可进一步增加研究结果的可靠性和准确度。另外,本研究还通过对7种原研制剂中8个模型药物的体外经皮渗透性研究,获得了常用动物皮肤模型(裸鼠、小型猪)中药物经皮渗透吸收速率与临床释药速率之间的比例关系。本研究为经皮给药系统研究的皮肤模型选择提供了科学依据,表明经过规范有效质控的离体猪皮是理想的体外试验皮肤模型。Animal skins,one kind of necessary study materials,play an important role in the development of transdermal products.The barrier characteristics of skins should be considered.The ~3HO in vitro transdermal permeability and transepidermal water loss(TEWL) are effective methods and important indicators for evaluating the barrier function of skins.The results showed that the freshness,thickness,mass and steady-state TEWL were the critical quality control points of the skin model,which could further improve the reliability and accuracy of the research results.In addition,the in vitro transdermal permeability tests of total eight model drugs from seven brand-name drugs were carried out to evaluate the correlation of the permeability rate in common animal skin models(nude mouse and mini pig skins) and the drug release rate in clinical practice.This study provided a scientific basis in selecting skin model and its results indicated that pig skin,under strict quality control,was preferred to be used in predicting the pharmacokinetics profiles of transdermal products.

关 键 词：经皮给药 动物皮肤模型 体外经皮渗透 经皮水分蒸发 质量控制 

分 类 号：R944.9[医药卫生—药剂学]