本文選題：芒果苷 + 固體分散體��； 參考：《中國醫(yī)院藥學雜志》2017年11期

【摘要】：目的:制備芒果苷(MGF)聚乙烯吡咯烷酮(PVP)固體分散體(MGF-SD),提高MGF的溶解度和溶出速度,并對比考察MGF、MGF-SD在體外腸道菌群模型中的代謝差異。方法:以PVP為載體材料,采用共沉淀法制備MGF固體分散體,通過差示掃描量熱法(DSC)、X射線粉末衍射法(XRD)和紅外光譜(IR)表征其物相特征。采用搖瓶法測定MGF、MGF-SD溶解度。采集健康志愿者新鮮糞便,制備腸道菌群混懸液,分別與MGF、MGF-SD在厭氧環(huán)境下孵育,HPLC法監(jiān)測MGF含量變化。結果:當MGF與PVP的質量比分別為1∶2,1∶4,1∶9時,MGF溶解度分別提高了432,513,633倍。DSC、XRD和IR均顯示,MGF-SD中MGF晶體結構發(fā)生破壞,以非晶狀態(tài)存在。體外釋放度測定結果表明,MGF-SD中MGF釋放速度快于MGF原料。與MGF原料相比,MGF制備成固體分散體后,離體人腸道菌群對MGF的代謝速度降低。結論:MGF制備成PVP固體分散體后,MGF以非晶型分子狀態(tài)高度分散在載體材料中,MGF溶出度與溶解度顯著提高,同時可減慢腸道菌群對MGF的代謝,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.
【作者單位】： 廣西衛(wèi)生職業(yè)技術學院;廣西中醫(yī)藥大學;廣西中醫(yī)藥大學中藥制劑共性技術研發(fā)重點實驗室;廣西醫(yī)科大學;廣西中醫(yī)藥大學制藥廠;
【基金】：廣西自然科學基金項目(編號:2014GXNSFAA118198) 國家自然科學基金項目(編號:81560674) 廣西高�？萍紕�(chuàng)新能力提升項目(編號:70-ZJGX201401002) 廣西中藥藥效研究重點實驗室系統(tǒng)性研究課題(編號:14-A-03-01)
【分類號】：R943;R96
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本文編號：1798768