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自乳化药物传递系统的最新进展:系统专利回顾(2011-2020 年)。

Recent Progress in Self-Emulsifying Drug Delivery Systems: A Systematic Patent Review (2011-2020).

机构信息

Departamento de Farmacia, Facultad de Ciencias, Universidad Nacional de Colombia, Bogotá D.C., Colombia.

Pharmacy Department, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil.

出版信息

Crit Rev Ther Drug Carrier Syst. 2022;39(2):1-77. doi: 10.1615/CritRevTherDrugCarrierSyst.2021038490.

DOI:10.1615/CritRevTherDrugCarrierSyst.2021038490
PMID:35378013
Abstract

Self-emulsifying drug delivery systems (SEDDS) are lipid-based isotropic mixtures that enhance the bioavailability of poorly water-soluble drugs and reduce the possible side effects, offering a wide variety of treatments for several pathologies. The aim of this review is to discuss the state of the art of patents for this drug delivery system by studying recent patent applications (2011 to 2020). We performed a thorough screening using the European Patent Office's Espacenet database, from which 37 inventions were selected and fully studied. China had more patent applications, and the articles published about SEDDS exceeds both in number and technological advance the submitted inventions. Nevertheless, the patents presented herein are innovative to address known issues to traditional SEDDS, including storage and formulation stability, solid formulations, acute gastrointestinal toxicity from surfactants, and drug delivery through alternative routes of administration. This study also revealed that release behavior for SEDDS and associated pharmacokinetics were not completely disclosed by the inventors of the patents and that further studies are required.

摘要

自乳化药物传递系统(SEDDS)是一种基于脂质的各向同性混合物,可提高疏水性药物的生物利用度并降低可能的副作用,为多种疾病提供了广泛的治疗选择。本综述旨在通过研究最近的专利申请(2011 年至 2020 年),讨论该药物传递系统的专利现状。我们使用欧洲专利局的 Espacenet 数据库进行了全面筛选,从中选择了 37 项发明并进行了全面研究。中国的专利申请较多,关于 SEDDS 的已发表文章在数量和技术进步方面都超过了提交的发明。然而,本文所介绍的专利具有创新性,可以解决传统 SEDDS 中的已知问题,包括储存和配方稳定性、固体配方、表面活性剂的急性胃肠道毒性以及通过替代给药途径的药物传递。这项研究还表明,SEDDS 的释放行为和相关药代动力学并未被专利发明人完全披露,需要进一步研究。

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