公开(公告)号：US20230372375A1

公开(公告)日：2023-11-23

申请号：US18029062

申请日：2020-09-30

申请人： Beijing Creatron Institute of Pharmaceutical Research Co. Ltd.

发明人： Huijuan JIA ,  Wei HOU ,  Yanxin WANG ,  Yan LI ,  Xiaohui REN ,  Tiange JIA

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.

公开(公告)号：US20230310393A1

公开(公告)日：2023-10-05

申请号：US17630709

申请日：2020-12-07

申请人： Tianjin Creatron Biotechnology Co., Ltd. ,  Beijing Creatron Institute of Pharmaceutical Research Co. Ltd.

发明人： Huijuan JIA ,  Jiayan ZHANG ,  Xin HOU ,  Yan LI

IPC分类号： A61K31/44 ,  A61K9/20 ,  A61K9/00

CPC分类号： A61K31/44 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/0053

摘要： A sorafenib pharmaceutical composition with high bioavailability and use thereof, and specifically a low-dose sorafenib oral solid preparation, comprising: a) a sorafenib solid dispersion; b) a crystallization inhibitor; and c) additional pharmaceutically acceptable adjuvant. The low-dose sorafenib oral solid preparation has high bioavailability and reduces the dosage of sorafenib such that the same therapeutic effect as that of Nexavar tablets can be achieved when a patient takes orally 35% to 70% of the administered dose of Nexavar tablets; it has higher stability, better safety, and less incidence of side effects; it has lower Cmax and AUC0-t variation, a higher dissolution, and a low crystal precipitation rate with the increase of pH in the gastrointestinal tract; it is easy to be taken by patients due to the small volume of the tablet; it has a fast disintegration speed and a good dissolution effect; and it is easy to realize industrialization.