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共无定形辛伐他汀-格列齐特的理化性质

Physicochemical characteristics of coamorphous simvastatin-gliclazide

  • 摘要: 制备共无定形辛伐他汀-格列齐特,对其溶出特性和物理稳定性进行了考察。结果证实产物为单相无定形态,辛伐他汀可能通过O-H与格列齐特磺酰脲基的C=O产生氢键相互作用,使通过常规方法难以制备成无定形的格列齐特实现了无定形化。共无定形物的形成显著提高了格列齐特的溶解度和溶出度,但对辛伐他汀无明显影响。与无定形辛伐他汀相比,该共无定形物的物理稳定性显著提高。

     

    Abstract: In this study, coamorphous simvastatin-gliclazide was prepared and characterized. Its single-phase amorphous nature was demonstrated. The hydrogen bond between the O-H group of simvastatin and sulfonylurea C=O group of gliclazide was revealed to be the trigger for the amorphization of gliclazide, which is difficult to form an amorphous state in other methods. Coamorphous simvastatin-gliclazide can significantly enhance the solubility and dissolution of gliclazide, without obvious effect on simvastatin. Compared with amorphous simvastatin, coamorphous simvastatin-gliclazide showed improved physical stability in the cunrent study.

     

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