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The Scientific World Journal
Volume 2013 (2013), Article ID 306476, 3 pages
http://dx.doi.org/10.1155/2013/306476
Research Article

Preparation and Cyclodextrin Solubilization of the Antibacterial Agent Benzoyl Metronidazole

School of Pharmacy, Ningxia Medical University, Yinchuan, Ningxia 750004, China

Received 24 April 2013; Accepted 25 June 2013

Academic Editors: A. Sacchetti, A. K. Saikia, and A. Sirit

Copyright © 2013 Qing Huang et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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 (  g/L) was substantially increased 9.7-fold (  g/L) by formation of 1 : 1 benzoyl metronidazole/β-cyclodextrin complexes in water, and the association constant value was determined to be 251 (±23) dm3/mol. Therefore, β-cyclodextrin can work as a pharmaceutical solubilizer for benzoyl metronidazole and may improve its oral bioavailability.