Ezetimibe and maleic acid pharmaceutical co-crystal and preparation method thereof

The invention discloses an ezetimibe co-crystal and a preparation method thereof, particularly relates to an ezetimibe and maleic acid pharmaceutical co-crystal and a preparation method thereof and belongs to the technical field of pharmaceutical co-crystals. The ezetimibe and maleic acid co-crystal...

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Bibliographische Detailangaben
Hauptverfasser: HU YANJIE, ZHANG FANGJIE, CHEN SHUIKU, LI YUNLI, YU YUZHEN, LI WEN, ZHU CHENGGONG, WANG RONGRONG, LI ZHANJUN, ZHANG XIAOHUI, LIU HONGMIN, HAO PINGPING
Format: Patent
Sprache:eng
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Zusammenfassung:The invention discloses an ezetimibe co-crystal and a preparation method thereof, particularly relates to an ezetimibe and maleic acid pharmaceutical co-crystal and a preparation method thereof and belongs to the technical field of pharmaceutical co-crystals. The ezetimibe and maleic acid co-crystal is formed with ezetimibe as an active pharmaceutical ingredient (API) and maleic acid as a co-crystal forerunner (CCF). The ezetimibe and the maleic acid are placed into a ball mill in a certain proportion and jointly ground to obtain the ezetimibe and maleic acid pharmaceutical co-crystal by adding a trace of alcohol solvent through a solid-state grinding method. The prepared ezetimibe and maleic acid co-crystal is subjected to structural characterization through P-XRD, DSC, IR and SEM, and the melting point of the co-crystal ranges from 110 DEG C to 114 DEG C. The solubility and dissolution rate of the ezetimibe co-crystal prepared through the method are obviously increased. By means of the method, only a little solvent is needed, few by-products are produced, operation is easy and convenient, and the method can be easily applied to industrial pharmacy and meets the requirement for environmental protection.