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Co-amorphous systems for the delivery of poorly water-soluble drugs: recent advances and an update.
Expert Opinion on Drug Delivery ( IF 5.0 ) Pub Date : 2020-09-17 , DOI: 10.1080/17425247.2020.1796631
Jiawei Han 1 , Yuanfeng Wei 1 , Yan Lu 1 , Runze Wang 1 , Jianjun Zhang 2 , Yuan Gao 1 , Shuai Qian 1
Affiliation  

ABSTRACT

Introduction

Most new drug candidates under development are poorly water-soluble, which are related to multiple pharmaceutical issues, increasing the bioavailability of these drugs by the improvement of solubility/dissolution has become a major concern to develop efficacious drugs with reasonable dosing regimens for patients. Over the past decade, increasing reports have been published on the investigation of co-amorphous drug delivery systems, with positive and excited outcomes in improving in vitro and in vivo performances of poorly water-soluble drugs.

Areas covered

This review summarizes recent findings of co-amorphous systems and provides their updates as a comprehensive overview in terms of classification, co-formers selection, preparation methods, physicochemical characteristics and in vivo performances.

Expert opinion

Co-amorphous system, a homogeneous single-phase system containing two compatible drugs or a drug with a pharmaceutically acceptable small-molecule co-former, has been employed as a promising formulation technology to improve in vitro and in vivo performances of poorly water-soluble drugs such as solubility/dissolution, stability, mechanical properties and bioavailability. Furthermore, a deeper understanding of co-amorphous systems, including its detailed classification, the criteria of co-former selection, stability mechanisms and the faced challenges as well as perspectives, will be more conducive to its development and application.



中文翻译:

用于输送水溶性差的药物的共非晶系统:最新进展和更新。

摘要

介绍

正在开发的大多数新候选药物水溶性差,这与多种药物问题有关,通过改善溶解度/溶解度来提高这些药物的生物利用度已成为开发具有合理剂量方案的有效药物的主要关注对象。在过去的十年中,关于共非晶药物递送系统的研究已发表了越来越多的报告,在改善水溶性差的药物的体外体内性能方面取得了积极和令人兴奋的结果。

覆盖区域

这篇综述总结了共非晶系统的最新发现,并就分类,共形成物的选择,制备方法,理化特性和体内性能等方面提供了其更新,作为一个全面的概述。

专家意见

共非晶体系,包含两种相容药物或具有可药用小分子共形成剂的药物的均相单相体系已被用作改善水溶性差的体外体内性能的有前途的制剂技术药物,例如溶解度/溶解度,稳定性,机械性能和生物利用度。此外,对共非晶系统的更深入的理解,包括其详细的分类,共形成者的选择标准,稳定性机制以及所面临的挑战和观点,将更有助于其发展和应用。

更新日期:2020-11-09
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