Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate

Metronidazole (MTZ) is an antibacterial drug widely used for the treatment of protozoan and anaerobic infections in humans and animals. However, its low bioavailability necessitates the frequent administration of a high dose to attain an effective plasma concentration profile for therapy. To reduce...

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Detalles Bibliográficos
Autores principales: Li, Jinhui, Hao, Xinghui, Wang, Chenguang, Liu, Haiyan, Liu, Lianchao, He, Xin, Sun, Changquan Calvin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8070254/
https://www.ncbi.nlm.nih.gov/pubmed/33919704
http://dx.doi.org/10.3390/pharmaceutics13040546
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author Li, Jinhui
Hao, Xinghui
Wang, Chenguang
Liu, Haiyan
Liu, Lianchao
He, Xin
Sun, Changquan Calvin
author_facet Li, Jinhui
Hao, Xinghui
Wang, Chenguang
Liu, Haiyan
Liu, Lianchao
He, Xin
Sun, Changquan Calvin
author_sort Li, Jinhui
collection PubMed
description Metronidazole (MTZ) is an antibacterial drug widely used for the treatment of protozoan and anaerobic infections in humans and animals. However, its low bioavailability necessitates the frequent administration of a high dose to attain an effective plasma concentration profile for therapy. To reduce the dose of MTZ, we have prepared a new cocrystal between MTZ and ethyl gallate (EG). The solid-state properties of MTZ-EG were characterized using complimentary techniques, including thermal, spectroscopic, microscopic, and X-ray crystallographic methods. The MTZ-EG cocrystal exhibits a higher solubility and faster dissolution than MTZ. The bioavailability of MTZ in rats was increased by 36% when MTZ-EG was used.
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spelling pubmed-80702542021-04-26 Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate Li, Jinhui Hao, Xinghui Wang, Chenguang Liu, Haiyan Liu, Lianchao He, Xin Sun, Changquan Calvin Pharmaceutics Article Metronidazole (MTZ) is an antibacterial drug widely used for the treatment of protozoan and anaerobic infections in humans and animals. However, its low bioavailability necessitates the frequent administration of a high dose to attain an effective plasma concentration profile for therapy. To reduce the dose of MTZ, we have prepared a new cocrystal between MTZ and ethyl gallate (EG). The solid-state properties of MTZ-EG were characterized using complimentary techniques, including thermal, spectroscopic, microscopic, and X-ray crystallographic methods. The MTZ-EG cocrystal exhibits a higher solubility and faster dissolution than MTZ. The bioavailability of MTZ in rats was increased by 36% when MTZ-EG was used. MDPI 2021-04-14 /pmc/articles/PMC8070254/ /pubmed/33919704 http://dx.doi.org/10.3390/pharmaceutics13040546 Text en © 2021 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
Li, Jinhui
Hao, Xinghui
Wang, Chenguang
Liu, Haiyan
Liu, Lianchao
He, Xin
Sun, Changquan Calvin
Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate
title Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate
title_full Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate
title_fullStr Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate
title_full_unstemmed Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate
title_short Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate
title_sort improving the solubility, dissolution, and bioavailability of metronidazole via cocrystallization with ethyl gallate
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8070254/
https://www.ncbi.nlm.nih.gov/pubmed/33919704
http://dx.doi.org/10.3390/pharmaceutics13040546
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