芒果苷PVP固体分散体的制备和表征及在体外肠道菌群模型中的代谢

发布时间：2018-04-24 23:32

  本文选题：芒果苷 + 固体分散体　； 参考：《中国医院药学杂志》2017年11期

【摘要】：目的:制备芒果苷(MGF)聚乙烯吡咯烷酮(PVP)固体分散体(MGF-SD),提高MGF的溶解度和溶出速度,并对比考察MGF、MGF-SD在体外肠道菌群模型中的代谢差异。方法:以PVP为载体材料,采用共沉淀法制备MGF固体分散体,通过差示扫描量热法(DSC)、X射线粉末衍射法(XRD)和红外光谱(IR)表征其物相特征。采用摇瓶法测定MGF、MGF-SD溶解度。采集健康志愿者新鲜粪便,制备肠道菌群混悬液,分别与MGF、MGF-SD在厌氧环境下孵育,HPLC法监测MGF含量变化。结果:当MGF与PVP的质量比分别为1∶2,1∶4,1∶9时,MGF溶解度分别提高了432,513,633倍。DSC、XRD和IR均显示,MGF-SD中MGF晶体结构发生破坏,以非晶状态存在。体外释放度测定结果表明,MGF-SD中MGF释放速度快于MGF原料。与MGF原料相比,MGF制备成固体分散体后,离体人肠道菌群对MGF的代谢速度降低。结论:MGF制备成PVP固体分散体后,MGF以非晶型分子状态高度分散在载体材料中,MGF溶出度与溶解度显著提高,同时可减慢肠道菌群对MGF的代谢,有利于提高MGF口服生物利用度。
[Abstract]:Aim: to prepare MGF-SDN, a solid dispersion of mangiferin (MGF) polyvinylpyrrolidone (PVP), to improve the solubility and dissolution rate of MGF, and to compare the metabolic differences of MGF MGF-SD in intestinal microflora model in vitro. Methods: PVP solid dispersion was prepared by coprecipitation method. The phase characteristics of MGF were characterized by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD) and infrared spectroscopy (IR). The solubility of MGF- MGF-SD was determined by shaking flask method. Fresh feces of healthy volunteers were collected to prepare intestinal microflora suspension and incubated with MGFMGF-SD in anaerobic environment to detect the changes of MGF content. Results: when the mass ratio of MGF to PVP was 1: 2, 1: 41: 9, the solubility of MGF increased 432513633 times. DSC-XRD and IR showed that the structure of MGF in MGF-SD was destroyed, and the structure was amorphous. The release rate of MGF in MGF-SD was faster than that of MGF. Compared with the raw material of MGF, the metabolism rate of MGF in isolated human intestinal microflora was decreased after the preparation of solid dispersion. Conclusion the dissolution and solubility of PVP were significantly increased after the preparation of PVP solid dispersion in amorphous molecular state, and the metabolism of MGF in intestinal microflora was slowed down, which was beneficial to the improvement of oral bioavailability of MGF.
【作者单位】： 广西卫生职业技术学院;广西中医药大学;广西中医药大学中药制剂共性技术研发重点实验室;广西医科大学;广西中医药大学制药厂;
【基金】：广西自然科学基金项目(编号:2014GXNSFAA118198) 国家自然科学基金项目(编号:81560674) 广西高校科技创新能力提升项目(编号:70-ZJGX201401002) 广西中药药效研究重点实验室系统性研究课题(编号:14-A-03-01)
【分类号】：R943;R96
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本文编号：1798768