4.7 Article

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

Journal

PHARMACEUTICS
Volume 13, Issue 4, Pages -

Publisher

MDPI
DOI: 10.3390/pharmaceutics13040546

Keywords

metronidazole; ethyl gallate; cocrystal; solubility; dissolution; pharmacokinetics

Funding

  1. Hebei Education Department [ZD2019109]
  2. Hebei Provincial Department of Science and Technology [19227505D]
  3. National Natural Science Foundation of China [32002326]

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The bioavailability of MTZ can be significantly increased and the drug dosage reduced by preparing a new cocrystal between MTZ and EG.
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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