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目的:以羟丙甲基纤维素琥珀酸酯(HAS)为载体材料制备吲达帕胺结肠定位释药微球并考察其体外释放度。方法:根据球晶造粒技术,采用乳化溶剂扩散法制备微球,以收率、载药量、包封率为优化指标,对影响微球制备的因素进行正交试验,通过神经网络遗传算法优选处方及工艺,并对以优化方案制备的微球进行了质量评价。结果:制备的吲达帕胺结肠定位释药微球形态圆整,大小均匀、表面光滑,粒径在50~250μm范围的微球占到92.07%,载药量为15.30%,包封率为95.48%;体外释药试验中,微球在模拟全胃肠不同pH条件下,即先在pH1.2和pH6.8介质中5 h累计释药17.54%,继在pH7.8介质中7 h后累积释药99.75%。结论:本试验筛选的处方及制备工艺可用于制备吲达帕胺结肠微球,且制备的微球能达到结肠定位释药的目的。
OBJECTIVE: To prepare colon-specific release microspheres of indapamide with hydroxypropyl methylcellulose succinate (HAS) as carrier material and investigate its in vitro release. Methods: According to the spherulite granulation technology, the microspheres were prepared by the emulsion solvent diffusion method. The yield, drug loading and entrapment efficiency were optimized. The factors affecting the preparation of the microspheres were studied by orthogonal experiments. The neural network genetic algorithm The prescriptions and processes were optimized, and the quality of microspheres prepared by optimization was evaluated. Results: The prepared indapamide colon-specific drug delivery microspheres were round, uniform in size and smooth in surface. The diameter of the microspheres in the range of 50 ~ 250μm accounted for 92.07% and the drug loading was 15.30% 95.48%. In in vitro drug release test, the microspheres in the simulated total gastrointestinal pH conditions, that is, first in pH1.2 and pH6.8 medium 5h cumulative release of 17.54%, followed by pH7.8 medium 7 h After the cumulative release of 99.75%. Conclusion: The prescription and preparation process of this experiment can be used to prepare indapamide colon microspheres, and the prepared microspheres can achieve the purpose of colonic colonization and drug release.