Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate
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...
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MDPI AG
2021-04-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/4/546 |
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| author | Jinhui Li Xinghui Hao Chenguang Wang Haiyan Liu Lianchao Liu Xin He Changquan Calvin Sun |
| author_facet | Jinhui Li Xinghui Hao Chenguang Wang Haiyan Liu Lianchao Liu Xin He Changquan Calvin Sun |
| author_sort | Jinhui Li |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-10T12:21:19Z |
| format | Article |
| id | doaj.art-83e4c09cff2244659e51ad376477de30 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T12:21:19Z |
| publishDate | 2021-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-83e4c09cff2244659e51ad376477de302023-11-21T15:30:09ZengMDPI AGPharmaceutics1999-49232021-04-0113454610.3390/pharmaceutics13040546Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl GallateJinhui Li0Xinghui Hao1Chenguang Wang2Haiyan Liu3Lianchao Liu4Xin He5Changquan Calvin Sun6College of Veterinary Medicine, Hebei Agricultural University, Baoding 071000, ChinaCollege of Veterinary Medicine, Hebei Agricultural University, Baoding 071000, ChinaPharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USACollege of Science, Hebei Agricultural University, Baoding 071000, ChinaCollege of Veterinary Medicine, Hebei Agricultural University, Baoding 071000, ChinaCollege of Veterinary Medicine, Hebei Agricultural University, Baoding 071000, ChinaPharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USAMetronidazole (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.https://www.mdpi.com/1999-4923/13/4/546metronidazoleethyl gallatecocrystalsolubilitydissolutionpharmacokinetics |
| spellingShingle | Jinhui Li Xinghui Hao Chenguang Wang Haiyan Liu Lianchao Liu Xin He Changquan Calvin Sun Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate Pharmaceutics metronidazole ethyl gallate cocrystal solubility dissolution pharmacokinetics |
| title | Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate |
| title_full | Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate |
| title_fullStr | Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate |
| title_full_unstemmed | Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate |
| title_short | Improving the Solubility, Dissolution, and Bioavailability of Metronidazole via Cocrystallization with Ethyl Gallate |
| title_sort | improving the solubility dissolution and bioavailability of metronidazole via cocrystallization with ethyl gallate |
| topic | metronidazole ethyl gallate cocrystal solubility dissolution pharmacokinetics |
| url | https://www.mdpi.com/1999-4923/13/4/546 |
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