Issue 11, 2022

Enhancing the stability of active pharmaceutical ingredients by the cocrystal strategy

Abstract

Cocrystallization has been recognized as one of the most successful approaches to address the stability problems of active pharmaceutical ingredients (APIs) in the past few decades. However, scant attention has been paid to the molecular mechanism of the enhanced stability, primarily due to the complicated degradation pathway and insufficient structural analysis. In this review, we would like to demonstrate that stable cocrystals have their roots in tailored design, delicate modification, and ingenious construction rather than luck. It is not only possible but also necessary to propose an individual cocrystal strategy to minimize the disadvantageous influence of environmental factors (heat, moisture, light, and oxygen). Therefore, a multidimensional structural understanding of the improved stability, including the manipulation of interaction strength, molecular conformation, packing styles, and electronic effect, has been provided here. Prominent examples of cocrystals that had successfully dealt with the same kinds of stability problems are summarized separately, revealing the vital structural factors in different scenarios and further paving the way for future stable cocrystal design.

Graphical abstract: Enhancing the stability of active pharmaceutical ingredients by the cocrystal strategy

Article information

Article type
Highlight
Submitted
30 Sept. 2021
Accepted
05 Janv. 2022
First published
13 Janv. 2022

CrystEngComm, 2022,24, 2002-2022

Enhancing the stability of active pharmaceutical ingredients by the cocrystal strategy

L. Liu, J. Wang and X. Mei, CrystEngComm, 2022, 24, 2002 DOI: 10.1039/D1CE01327K

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements