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推进对片剂崩解现象的理解 - 近期研究进展。

Advancing the understanding of the tablet disintegration phenomenon - An update on recent studies.

机构信息

Department of Pharmaceutical Sciences and Pharmaceutics Faculty of Pharmacy, Applied Science Private University, Amman 11931, Jordan.

Department of Pharmaceutics and Pharmaceutical Technology, School of Pharmacy, The University of Jordan, Amman 11942, Jordan.

出版信息

Int J Pharm. 2021 Apr 1;598:120390. doi: 10.1016/j.ijpharm.2021.120390. Epub 2021 Feb 16.

DOI:10.1016/j.ijpharm.2021.120390
PMID:33607196
Abstract

Disintegration is the de-aggregation of particles within tablets upon exposure to aqueous fluids. Being an essential step in the bioavailability cascade, disintegration is a fundamental quality attribute of immediate release tablets. Although the disintegration phenomenon has been studied for over six decades, some gaps of knowledge and research questions still exist. Three reviews, published in 2015, 2016 and 2017, have discussed the literature relative to tablet disintegration and summarised the understanding of this topic. Yet, since then more studies have been published, adding to the established body of knowledge. This article guides a step forward towards the comprehension of disintegration by reviewing, concisely, the most recent scientific updates on this topic. Initially, we revisit the mechanisms of disintegration with relation to the three most used superdisintegrants, namely sodium starch glycolate, croscarmellose sodium and crospovidone. Then, the influence of formulation, storage, manufacturing and media conditions on disintegration is analysed. This is followed by an excursus on novel disintegrants. Finally, we highlight unanswered research questions and envision future research venues in the field.

摘要

崩解是片剂在暴露于水液时颗粒的离析。作为生物利用度级联中的一个基本步骤,崩解是速释片剂的一个基本质量属性。尽管崩解现象已经研究了六十多年,但仍存在一些知识空白和研究问题。三篇综述于 2015 年、2016 年和 2017 年发表,讨论了与片剂崩解相关的文献,并总结了对这一主题的理解。然而,自那时以来,更多的研究已经发表,增加了已建立的知识体系。本文通过回顾最近关于这个主题的科学更新,朝着理解崩解的方向迈进了一步。首先,我们简要回顾与三种最常用的超级崩解剂(即交联羧甲基淀粉钠、交联聚维酮和羧甲基淀粉钠)相关的崩解机制。然后,分析了配方、储存、制造和介质条件对崩解的影响。接下来是对新型崩解剂的探讨。最后,我们强调了未解决的研究问题,并设想了该领域未来的研究方向。

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