SGLT-2 INHIBITOR SARCOSINE CO-CRYSTAL, PREPARATION METHOD THEREFOR AND USE THEREOF

    公开(公告)号:US20230372375A1

    公开(公告)日:2023-11-23

    申请号:US18029062

    申请日:2020-09-30

    IPC分类号: A61K31/7042 A61K31/198

    CPC分类号: A61K31/7042 A61K31/198

    摘要: Provided are an SGLT-2 inhibitor-sarcosine cocrystal, a preparation method therefor and use thereof. Using sarcosine as a ligand, said cocrystal has higher safety and lower costs; a drug cocrystal has higher stability, and during the production process or storage process of a formulation composition, the crystal form is not easily changed; said cocrystal does not melt when heated, does not stick, aggregate or generate static electricity, and has better mixing uniformity. Said cocrystal has uniform distribution in a prepared pharmaceutical composition, causing that the pharmaceutical composition has better in-vivo release, absorption and efficacy, and has small difference between batches; and the pharmaceutical composition has high stability, and is more conducive to storage and transportation. The present invention has a simple preparation process, has high reproducibility, has short crystallization time, has low process condition requirements, and has higher economic benefits; the present invention does not use an unsafe solvent during the preparation process; and a crude product or intermediate of the SGLT-2 inhibitor can be simultaneously purified.