title: Preparation and cyclodextrin solubilization of the antibacterial agent benzoyl metronidazole.
abstract: A one-pot method for the preparation of benzoyl metronidazole was achieved by using N,N'-carbonyldiimidazole as a coupling reagent. Moreover, it was found that the byproduct imidazole as the catalyst promoted the reaction. In addition, the β-cyclodextrin solubilization of benzoyl metronidazole was investigated by phase-solubility method. The phase-solubility studies indicated that the solubility of benzoyl metronidazole (S = 0.1435 g/L) was substantially increased 9.7-fold (S' = 1.3881 g/L) by formation of 1 : 1 benzoyl metronidazole/β-cyclodextrin complexes in water, and the association constant K(a) value was determined to be 251 (±23) dm(3)/mol. Therefore, β-cyclodextrin can work as a pharmaceutical solubilizer for benzoyl metronidazole and may improve its oral bioavailability.
authors: School of Pharmacy, Ningxia Medical University, Yinchuan, Ningxia 750004, China.
authors: Qing
authors: Q
authors: Huang
authors: Benpeng
authors: B
authors: Li
authors: Shuo
authors: S
authors: Yang
authors: Peipei
authors: P
authors: Ma
authors: Zhizhong
authors: Z
authors: Wang
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry*; D003505:Cyclodextrins / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008795:Metronidazole / Q000031:analogs & derivatives / Q000737:chemistry*; D012995:Solubility
chemical_list: D000900:Anti-Bacterial Agents; D003505:Cyclodextrins; D008795:Metronidazole
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