Abstract:

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 wa? ter，degradation and characteristics of biocompatibility. The chemical structures of the controlled?release preparation were charac? terized 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 con? ditions of molar ratio of 3∶1，ultrasonic power of 400 W，and reaction time of 200 s. The solubility of the controlled?release prepa? ration in water increased to 18.99 mg/ml. There was 40% metronidazole released in 12 h in buffer solution. Conclusion A new controlled?release preparation of metronidazole is synthesized successfully by using sodium alginate and its release rate is satisfac? tory.

摘要：

目的制备甲硝唑缓释药，提高甲硝唑水溶性和缓释效果。方法通过超声法用海藻酸钠包裹甲硝唑，制备甲硝唑缓释药，以红外光谱、核磁氢谱、差式扫描量热分析和扫描电镜表征该缓释药理化结构，根据国标测定其溶解度，并用紫外光分光光度法测定其包合率和缓释效果。结果本实验制得了一种甲硝唑缓释药，通过正交实验确定了最佳反应条件为：物料摩尔比3∶1、反应功率400 W、反应时间200 s。通过红外光谱、核磁氢谱、差式扫描量热分析和扫描电镜分析，确证该包合物为海藻酸钠包裹甲硝唑的产物。该缓释药溶解度可达18.99 mg/ml，体外释放结果表明12 h内甲硝唑的释放量达40%。结论用海藻酸钠包裹甲硝唑，成功制备了具有良好缓释效果的甲硝唑缓释药。

关键词: 甲硝唑；海藻酸钠；缓释；表征