[Synthesis and characterization of controlled-release preparation of metronidazole].
OBJECTIVE
To increase the solubility of metronidazole in water in order to increase its bioavailability.


METHODS
A new controlled-release preparation of metronidazole was synthesized by using sodium alginate which had good solubility in water, degradation and characteristics of biocompatibility. The chemical structures of the controlled-release preparation were characterized by FT-IR, 1H-NMR, DSC and SEM. The solubility was assayed according to the National Standard. The inclusion rate and controlled-release effect were assayed by UV spectrum.


RESULTS
The inclusion rate could reach maximum under the optimum conditions of molar ratio of 3:1, ultrasonic power of 400 W, and reaction time of 200 s. The solubility of the controlled-release preparation in water increased to 18.99 mg/ml. There was 40% metronidazole released in 12 h in buffer solution.


CONCLUSIONS
A new controlled-release preparation of metronidazole is synthesized successfully by using sodium alginate and its release rate is satisfactory.
School of Petrochemical Engineering, Changzhou University, Changzhou 213164, China.
Wei
W
Zhang
Qiang
Q
Chen
Xiao-Qiang
XQ
Sun
D000464:Alginates / Q000737:chemistry; D000871:Anthelmintics / Q000138:chemical synthesis* / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000138:chemical synthesis* / Q000737:chemistry; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D007700:Kinetics; D008795:Metronidazole / Q000138:chemical synthesis* / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared
D000464:Alginates; D000871:Anthelmintics; D003692:Delayed-Action Preparations; D006603:Hexuronic Acids; D008795:Metronidazole; D020723:Glucuronic Acid