【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。更多还原

【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.更多还原