Li Jinhui, Hao Xinghui, Wang Chenguang, Liu Haiyan, Liu Lianchao, He Xin, Sun Changquan Calvin
College of Veterinary Medicine, Hebei Agricultural University, Baoding 071000, China.
Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA.
Pharmaceutics. 2021 Apr 14;13(4):546. doi: 10.3390/pharmaceutics13040546.
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.
甲硝唑（MTZ）是一种广泛用于治疗人和动物原生动物及厌氧菌感染的抗菌药物。然而，其低生物利用度需要频繁高剂量给药才能获得有效的血浆浓度曲线以进行治疗。为了降低MTZ的剂量，我们制备了MTZ与没食子酸乙酯（EG）的新型共晶体。采用热分析、光谱分析、显微镜分析和X射线晶体学方法等多种互补技术对MTZ-EG的固态性质进行了表征。MTZ-EG共晶体比MTZ具有更高的溶解度和更快的溶解速度。使用MTZ-EG时，MTZ在大鼠体内的生物利用度提高了36%。
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