Improving the solubility, dissolution, and bioavailability of metronidazole via cocrystallization with ethyl gallate

Jinhui Li; Xinghui Hao; Chenguang Wang; Haiyan Liu; Lianchao Liu; Xin He; Changquan Calvin Sun

doi:10.3390/pharmaceutics13040546

Improving the solubility, dissolution, and bioavailability of metronidazole via cocrystallization with ethyl gallate

Jinhui Li, Xinghui Hao, Chenguang Wang, Haiyan Liu, Lianchao Liu, Xin He, Changquan Calvin Sun

Pharmaceutics

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18 Scopus citations

Abstract

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.

Original language	English (US)
Article number	546
Journal	Pharmaceutics
Volume	13
Issue number	4
DOIs	https://doi.org/10.3390/pharmaceutics13040546
State	Published - Apr 2021

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Publisher Copyright:
© 2021 by the authors. Licensee MDPI, Basel, Switzerland.

Keywords

Cocrystal
Dissolution
Ethyl gallate
Metronidazole
Pharmacokinetics
Solubility

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10.3390/pharmaceutics13040546

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abstract = "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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author = "Jinhui Li and Xinghui Hao and Chenguang Wang and Haiyan Liu and Lianchao Liu and Xin He and Sun, {Changquan Calvin}",

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T1 - Improving the solubility, dissolution, and bioavailability of metronidazole via cocrystallization with ethyl gallate

AU - Li, Jinhui

AU - Hao, Xinghui

AU - Wang, Chenguang

AU - Liu, Haiyan

AU - Liu, Lianchao

AU - He, Xin

AU - Sun, Changquan Calvin

PY - 2021/4

Y1 - 2021/4

N2 - 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.

AB - 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.

KW - Cocrystal

KW - Dissolution

KW - Ethyl gallate

KW - Metronidazole

KW - Pharmacokinetics

KW - Solubility

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ER -

Improving the solubility, dissolution, and bioavailability of metronidazole via cocrystallization with ethyl gallate

Abstract

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