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

Research output: Contribution to journalArticlepeer-review

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 languageEnglish (US)
Article number546
JournalPharmaceutics
Volume13
Issue number4
DOIs
StatePublished - Apr 14 2021

Bibliographical note

Funding Information:
Acknowledgments: We are grateful for the financial support of the Educational Commission of Hebei Province of China (ZD2019109) and Key R&D Program of Hebei Province (No. 19227505D).

Funding Information:
Funding: This research was funded by Hebei Education Department, grant number “ZD2019109” Hebei Provincial Department of Science and Technology, grant number “19227505D” and National Natural Science Foundation of China, grant number “32002326”.

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

Keywords

  • Cocrystal
  • Dissolution
  • Ethyl gallate
  • Metronidazole
  • Pharmacokinetics
  • Solubility

PubMed: MeSH publication types

  • Journal Article

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