Co-crystal of tegafur and syringic acid and preparation method thereof

The invention relates to the field of pharmaceutical co-crystals, and discloses a pharmaceutical co-crystal of tegafur and syringic acid and a preparation method thereof. The molecular formula of thepharmaceutical co-crystal is [C8H9FN2O3.C9H10O5], and a tegafur molecule and a syringic acid molecule...

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Hauptverfasser: YAN CUIWEI, WU ZHIYONG, LI YANTUAN, WANG LINGYANG, YU MINGCHAO
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to the field of pharmaceutical co-crystals, and discloses a pharmaceutical co-crystal of tegafur and syringic acid and a preparation method thereof. The molecular formula of thepharmaceutical co-crystal is [C8H9FN2O3.C9H10O5], and a tegafur molecule and a syringic acid molecule compose a basic structural unit of the co-crystal. The pharmaceutical co-crystal belongs to a monoclinic system, and the space group is P21/m. According to the method, tegafur and syringic acid are used as the raw materials for feeding according to a molar ratio of 1:1, and a solvent evaporation method and a cooling method are respectively adopted to prepare the stable pharmaceutical co-crystal in methanol. The pharmaceutical co-crystal provided by the invention improves the physicochemical properties of tegafur, and is conducive to exerting the synergistic anti-tumor activity of syringic acid and tegafur. The skeleton structure of the pharmaceutical co-crystal can still be maintained after long-term placement und