Cargando…

Recrystallization Mediates the Gelation of Amorphous Drugs: The Case of Acemetacin

Amorphization is widely used as an effective method of increasing the solubility of insoluble drugs. However, some amorphous drugs exhibit a much lower dissolution rate than their corresponding crystalline form due to their gelation. In this study, we reported the gels formed from amorphous acemetac...

Descripción completa

Detalles Bibliográficos
Autores principales: Teng, Manlin, Li, Jianfeng, Li, Zhaohua, Zhang, Guangshuai, Zhao, Peixu, Fu, Qiang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9860709/
https://www.ncbi.nlm.nih.gov/pubmed/36678848
http://dx.doi.org/10.3390/pharmaceutics15010219
_version_ 1784874653888544768
author Teng, Manlin
Li, Jianfeng
Li, Zhaohua
Zhang, Guangshuai
Zhao, Peixu
Fu, Qiang
author_facet Teng, Manlin
Li, Jianfeng
Li, Zhaohua
Zhang, Guangshuai
Zhao, Peixu
Fu, Qiang
author_sort Teng, Manlin
collection PubMed
description Amorphization is widely used as an effective method of increasing the solubility of insoluble drugs. However, some amorphous drugs exhibit a much lower dissolution rate than their corresponding crystalline form due to their gelation. In this study, we reported the gels formed from amorphous acemetacin (ACM) for the first time. Gelation was promoted at conditions of lower pH, higher temperature and lower ionic strength. Solid-state characterizations suggested that ACM gels may be formed by recrystallization. This mechanism provides a new direction in facilitating the elimination of gelation for amorphous drugs. Moreover, it also provides the basis for the development of sustained-release formulations using the gelation properties.
format Online
Article
Text
id pubmed-9860709
institution National Center for Biotechnology Information
language English
publishDate 2023
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-98607092023-01-22 Recrystallization Mediates the Gelation of Amorphous Drugs: The Case of Acemetacin Teng, Manlin Li, Jianfeng Li, Zhaohua Zhang, Guangshuai Zhao, Peixu Fu, Qiang Pharmaceutics Article Amorphization is widely used as an effective method of increasing the solubility of insoluble drugs. However, some amorphous drugs exhibit a much lower dissolution rate than their corresponding crystalline form due to their gelation. In this study, we reported the gels formed from amorphous acemetacin (ACM) for the first time. Gelation was promoted at conditions of lower pH, higher temperature and lower ionic strength. Solid-state characterizations suggested that ACM gels may be formed by recrystallization. This mechanism provides a new direction in facilitating the elimination of gelation for amorphous drugs. Moreover, it also provides the basis for the development of sustained-release formulations using the gelation properties. MDPI 2023-01-08 /pmc/articles/PMC9860709/ /pubmed/36678848 http://dx.doi.org/10.3390/pharmaceutics15010219 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Teng, Manlin
Li, Jianfeng
Li, Zhaohua
Zhang, Guangshuai
Zhao, Peixu
Fu, Qiang
Recrystallization Mediates the Gelation of Amorphous Drugs: The Case of Acemetacin
title Recrystallization Mediates the Gelation of Amorphous Drugs: The Case of Acemetacin
title_full Recrystallization Mediates the Gelation of Amorphous Drugs: The Case of Acemetacin
title_fullStr Recrystallization Mediates the Gelation of Amorphous Drugs: The Case of Acemetacin
title_full_unstemmed Recrystallization Mediates the Gelation of Amorphous Drugs: The Case of Acemetacin
title_short Recrystallization Mediates the Gelation of Amorphous Drugs: The Case of Acemetacin
title_sort recrystallization mediates the gelation of amorphous drugs: the case of acemetacin
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9860709/
https://www.ncbi.nlm.nih.gov/pubmed/36678848
http://dx.doi.org/10.3390/pharmaceutics15010219
work_keys_str_mv AT tengmanlin recrystallizationmediatesthegelationofamorphousdrugsthecaseofacemetacin
AT lijianfeng recrystallizationmediatesthegelationofamorphousdrugsthecaseofacemetacin
AT lizhaohua recrystallizationmediatesthegelationofamorphousdrugsthecaseofacemetacin
AT zhangguangshuai recrystallizationmediatesthegelationofamorphousdrugsthecaseofacemetacin
AT zhaopeixu recrystallizationmediatesthegelationofamorphousdrugsthecaseofacemetacin
AT fuqiang recrystallizationmediatesthegelationofamorphousdrugsthecaseofacemetacin