Solid dispersions (SDs) of glibenclamide (GBM); a poorly water-soluble drug and polyglycolized glycerides (Gelucire with the aid of silicon dioxide (Aerosil 200); as an adsorbent, were prepared by spray drying technique. SDs and spray dried GBM in comparison with pure GBM and corresponding physical mixtures (PMs) were initially characterized and then subjected to ageing study up to 3 months. Initial characterization of SDs and spray dried GBM by DSC and XRPD showed that GBM was present in its amorphous form (AGBM). Improvement in the solubility and dissolution rate was observed for all samples. DRIFT spectroscopy revealed presence of hydrogen bonding in SDs. During ageing study, almost no decrease of in vitro drug dissolution was observed, over the period of 3 months as compare with freshly prepared SDs. Slight crystallinity in SDs was observed in the DSC and XRPD studies during ageing. Moreover in vivo study in Swiss Albino mice also justified the improvement in the therapeutic efficacy of amorphous GBM in SDs over pure GBM. Thus, present study demonstrated the high potential of spray drying technique for obtaining stable free flowing SDs of poorly water-soluble drugs using polyglycolized glycerides carriers with the aid of silicon dioxide as an adsorbent.

译文

:格列苯脲(GBM)的固体分散体(SD);通过喷雾干燥技术制备了水溶性差的药物和聚乙二醇化甘油酯(Gelucire,借助二氧化硅(Aerosil 200)作为吸附剂),将SD和喷雾干燥的GBM与纯GBM和相应的物理混合物(PM)进行了比较首先进行了表征,然后进行了长达3个月的老化研究,通过DSC和XRPD对SD和喷雾干燥的GBM进行了初步表征,结果表明GBM以无定形形式存在(AGBM),并观察到所有化合物的溶解度和溶解速率均有所提高DRIFT光谱显示SD中存在氢键;在老化研究中,与新鲜制备的SD相比,在3个月的时间内几乎没有观察到体外药物溶解的减少;在DSC和DSC中观察到SD的结晶度较小在衰老过程中进行XRPD研究,此外,对瑞士白化病小鼠进行的体内研究也证明了无定形GBM在SD中的治疗效果优于纯GBM。目前的研究表明,喷雾干燥技术在使用聚乙二醇化甘油酯载体和二氧化硅作为吸附剂的情况下获得水溶性差的药物的稳定自由流动SD的潜力很大。

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