摘要:
目的: 探讨乳化交联法制备甲硝唑羧甲基壳聚糖微球的最佳工艺,并了解微球体外释药规律。 方法: 按正交设计,考察不同羧甲基壳聚糖浓度、投药比、交联度、乳化转速等条件对质量指标的影响,选出最佳方案,并进一步检测微球的体外释放特性。 结果: 各因素对所制微球综合评分指标的影响大小依次为:乳化转速>投药比>交联度>羧甲基壳聚糖浓度,用优化的工艺制得微球50-200μm粒径分布百分数为48.86%,载药量为48.19%,包封率为37.46%,在pH1.2、6.8和7.6,3种缓冲液中的释放时间为6-8h。 结论: 本法所制微球工艺稳定,在体外具有缓释作用。
Abstract:
Objective: To study the optimum technology for preparing metronidazole-loaded carboxymethyl chitosan（MZ-CMC） microspheres by emulsification and cross-linking process and to investigate the in-vitro release characteristics of MZ-CMC microspheres. Methods: An orthogonal test,based on 4 factors including CMC concentration,MZ/CMC（W/W）,glutaradehyde/CMC（W/W） and agitation speed,was employed to determine the optimum preparetion technology of microspheres.The in vitro release behavior was recorded and evaluated. Results: For this 4 factors,the degree of influence on the quality of microspheres were gradually lower in the sequence of "agitation speed","MZ/CMC（W/W）","glutaradehyde/CMC（W/W）",and "CMC concentration".Prepared with optimized method in this test,the proportion of microspheres with diameter from 50-200 μm was 48.86%.The drug content was 48.19%,and the enveloping rate was 37.46%.The in virto release time was from 6-8 h in 3 types of buffer solution of pH1.2,6.8 and 7.6. Conclusion: The preparing technology for MZ-CMC microspheres used in this test is dependable,and the in vitro release of MZ from the microspheres is sustained.
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