Co-crystals of fuqinotinib, methods of making, compositions, and uses thereof
By preparing a cocrystal of fruquintinib with saccharin, malonic acid, and maleic acid, the problem of crystallization process instability caused by the polymorphism of fruquintinib was solved, and a novel crystal form with high solubility, good fluidity, and strong stability was achieved, which is suitable for preparing drugs to treat diseases related to angiogenesis disorders.
Patent Information
- Application Number
- CN202310975265.2
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Filing Date
- 2018-03-30
- Publication Date
- 2026-02-06
- Estimated Expiration
- 2038-03-30
AI Technical Summary
The existing polymorphism of fruquintinib makes it difficult to obtain a single crystal form in the crystallization process, affecting process repeatability and product quality. Furthermore, the known crystal forms have poor flowability, low water solubility, and insufficient stability.
We developed a eutectic of fruquintinib with saccharin, malonic acid, and maleic acid, and prepared a novel crystal form with high solubility, good flowability, and strong stability using specific solvents and reaction conditions.
It improved the water solubility and bioavailability of fruquintinib, improved particle morphology and flowability, enhanced crystal stability and processability, and reduced quality and safety issues during drug production and storage.