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
Affiliations
Jinhui Li
College of Veterinary Medicine, Hebei Agricultural University, Baoding 071000, China
Xinghui Hao
College of Veterinary Medicine, Hebei Agricultural University, Baoding 071000, China
Chenguang Wang
Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA
Haiyan Liu
College of Science, Hebei Agricultural University, Baoding 071000, China
Lianchao Liu
College of Veterinary Medicine, Hebei Agricultural University, Baoding 071000, China
Xin He
College of Veterinary Medicine, Hebei Agricultural University, Baoding 071000, China
Changquan Calvin Sun
Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA
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.
