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

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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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Li, J., Hao, X., Wang, C., Liu, H., Liu, L., He, X., & Sun, C. C. (2021). Improving the solubility, dissolution, and bioavailability of metronidazole via cocrystallization with ethyl gallate. Pharmaceutics, 13(4). https://doi.org/10.3390/pharmaceutics13040546

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