ETORICOXIB SOLVATES AND PREPARATION METHOD THEREOF
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United States of America Patent
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Sep 30, 2021
app pub date -
Mar 22, 2021
filing date -
Mar 31, 2020
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Abstract
The disclosure relates to etoricoxib solvates and a preparation method thereof. A solvent is a hydrogen bond donor solvent with a polarity value π* ranging from 60 to 100 or a hydrogen bond acceptor solvent with a polarity value π* ranging from 92 to 100. Solvents with a polarity value π* within the above range all can form corresponding etoricoxib solvates with etoricoxib. The etoricoxib solvate can be prepared by cooling crystallization or suspension crystallization. A 1,2-propanediol solvate of etoricoxib and a dimethyl sulfoxide (DMSO) solvate of etoricoxib provided in the present disclosure have high thermal stability, unique crystal form, large size, concentrated distribution, and prominent flowability and is safe, pharmaceutically acceptable, and not easy to agglomerate. Compared with etoricoxib, the etoricoxib solvates exhibit significantly improved solubility. Moreover, preparation of the solvates requires low consumption in time, energy, and solvent, and has high efficiency, with a molar yield higher than 90%.
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