共无定形盐酸鲁拉西酮-莽草酸的稳定性研究

    Investigation on the Stability of Coamorphous Lurasidone Hydrochloride-shikimic Acid

    • 摘要: 目的 建立盐酸鲁拉西酮的含量测定方法,并对盐酸鲁拉西酮-莽草酸共无定形体系的稳定性进行研究。方法 采用溶剂法(真空减压旋转蒸发法)制备得到3种摩尔比为1:1,1:2及2:1的共无定形盐酸鲁拉西酮-莽草酸,采用熔点仪、偏光显微镜、HPLC、PXRD等方法对共无定形盐酸鲁拉西酮-莽草酸进行了理化性质的考察。结果 制备的3种共无定形盐酸鲁拉西酮-莽草酸中以摩尔比为1:2的共无定形最为稳定。结论 通过提高莽草酸的比例,可以在一定程度上提高共无定形的稳定性。

       

      Abstract: OBJECTIVE To establish a method for the determination of lurasidone hydrochloride and to study the stability of the lurasidone hydrochloride-shikimic acid coamorphous system. METHODS Three kinds of coamorphous lurasidone hydrochloride-shikimic acid with molar ratios of 1:1, 1:2 and 2:1 were prepared by the solvent method(vacuum and reduced pressure rotary evaporation method), using melting point instrument and polarizing microscope. The physical and chemical properties of the coamorphous lurasidone hydrochloride-shikimic acid were investigated by methods such as HPLC and PXRD. RESULTS Among the three prepared coamorphous lurasidone-shikimic acid, the coamorphous one with a molar ratio of 1:2 was the most stable. CONCLUSION By increasing the ratio of shikimic acid, the stability of the coamorphous form can be improved.

       

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