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目的 :考察甲硝唑微囊口服结肠定位给药系统的制备工艺。方法 :采用液中干燥法制备微囊 ,应用均匀试验设计 ,考察各因素水平对微囊包封率、载药量的影响。按优化后的结果选择实验条件 ,进行重复实验 ,用体外溶出实验考察其结肠定位释放效果。结果 :制备的甲硝唑微囊包封率为 ( 62 .3± 1.3 ) % ,载药量为 ( 5 9.8± 2 .0 ) % ,所制备的片剂在 0 .1mol·L- 1 盐酸溶液和 pH6.8磷酸盐缓冲液中几乎不释放 ,而在 pH7.5磷酸盐缓冲液中 3 0min的平均累积释放量为 82 .13 %。结论 :优化后的制备工艺对甲硝唑微囊口服结肠定位给药系统的研究和应用具有一定的参考价值。
Objective: To investigate the preparation of metronidazole microcapsules oral colon-specific delivery system. Methods: The microcapsules were prepared by the liquid drying method. The uniform design of the microcapsules was used to investigate the effect of the factors on the entrapment efficiency and drug loading of the microcapsules. Select the experimental conditions according to the optimized results, repeat the experiment, and investigate the releasing effect of colon colonization by in vitro dissolution experiment. Results: The encapsulation efficiency of metronidazole microcapsules was (62.3 ± 1.3)% and the drug loading was (5 9.8 ± 2.0)%. The prepared tablets were dissolved in 0.1 mol·L-1 hydrochloric acid Solution and pH 6.8 phosphate buffer, whereas the average cumulative release of 30 min in pH 7.5 phosphate buffer was 82.13%. Conclusion: The optimized preparation process has certain reference value for the study and application of oral administration of metronidazole microcapsules.