透皮贴剂渗透性研究进展  

Research Progress on Permeability of Transdermal Patches

作　　者：江霞 马迅[2,3] 刘万卉 陈华[2,3] Jiang Xia;Ma Xun;Liu Wanhui;Chen Hua(Yantai University,Yantai 264005,China;National Institutes for Food and Drug Control,Beijing 102629,China;NMPA Key Laboratory for Quality Research and Evaluation of Chemical Drugs,Beijing 102629,China)

机构地区：[1]烟台大学,烟台264005 [2]中国食品药品检定研究院,北京102629 [3]国家药品监督管理局化学药品质量研究与评价重点实验室,北京102629

出　　处：《中国药事》2023年第3期312-320,共9页Chinese Pharmaceutical Affairs

基　　金：中国食品药品检定研究院化学药品检定所学科建设基金项目(编号1030050090115)。

摘　　要：与传统注射剂和口服制剂相比,透皮贴剂具有避免首过消除效应、维持稳定的血药浓度以及提高患者的用药依从性等许多优势,其研发和产业化发展近年来受到了广泛的关注,但经皮吸收这一过程的存在使得透皮贴剂的生物利用度难以达到临床要求。因此,如何改善药物的经皮渗透以及如何评价药物的体外渗透成为透皮贴剂开发的关键和难点。本文结合国内外相关文献将现阶段透皮贴剂的促透方法及其机制进行归纳,为开发新的促透方法,提高药物的生物利用度提供思路;同时总结了体外渗透试验主要方法及常用皮肤模型、用于体外渗透分析的成像技术等,为解决目前关于透皮贴剂渗透性存在的诸多问题与挑战,制定更为完善的关于透皮贴剂渗透性的要求和标准提供参考。Compared with traditional injections and oral preparations, transdermal patches have many advantages, such as avoiding the fi rst-pass elimination ef fect, maintaining stable blood drug concentrations, and improving patients’ medication compliance. Their R&D and industrial development have received extensive attention in recent years, but the existence of the process of percutaneous absorption makes it difficult for the bioavailability of transdermal patches to meet clinical requirements. Therefore, how to improve the transdermal penetration of drugs and how to evaluate the in vitro penetration of drugs have become the key and difficult points in the development of transdermal patches. In this paper, the current penetration-enhancing methods and mechanisms of transdermal patches are summarized based on the relevant domestic and foreign literatures,providing ideas for developing new penetration-enhancing methods and improving the bioavailability of drugs.At the same time, this paper summarized the main methods, skin models commonly for in vitro penetration tests and imaging techniques for in vitro penetration analysis, etc, providing a reference for solving many problems and challenges existing in the permeability of transdermal patches and formulating more complete requirements and standards for the permeability of transdermal patches.

关 键 词：透皮贴剂 经皮吸收 促渗剂 体外渗透 FRANZ扩散池 

分 类 号：R917[医药卫生—药物分析学]