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Title:
NEW CRYSTAL FORMS OF DAPAGLIFLOZIN AND PREPARATION METHOD THEREOF
Document Type and Number:
WIPO Patent Application WO/2020/187150
Kind Code:
A1
Abstract:
Disclosed are new crystal forms of dapagliflozin and a preparation method thereof. Particularly, the X-ray powder diffraction pattern of the crystal form A of dapagliflozin has characteristic diffraction peaks at the following 2θ angles: 6.3±0.2°, 12.5±0.2°, 16.0±0.2°, 18.8±0.2°, 26.4±0.2°, and 27.1±0.2°. The X-ray powder diffraction pattern of the crystal form B of dapagliflozin has characteristic diffraction peaks at the following 2θ angles: 6.3±0.2°, 7.2±0.2°, 14.5±0.2°, 19.6±0.2°, 21.3±0.2°, and 23.6±0.2°. The crystal form A is hemi-ethanol solvate, which is stable when it is baked at 10-30℃. The ethanol solvent can be easily removed by baking at 45-55℃ to obtain the anhydrous crystal form B. The crystal form A is an intermediate state crystal form of the anhydrous crystal form B. At the same time, the crystal form A of hemi-ethanol solvate can be directly used in preparation by performing wet granulation and removing the solvent by baking, and can meet the quality requirements of the preparation. The crystal form B has a low water content, a high purity, a good product stability at 60℃ high temperature, a simple preparation process with mild operation conditions, and is suitable for large scale industrial production.

Inventors:
GE SHUWANG (CN)
HUANG JITING (CN)
TANG WEI (CN)
YANG WENQIAN (CN)
WANG TIE-LIN (CN)
Application Number:
PCT/CN2020/079204
Publication Date:
September 24, 2020
Filing Date:
March 13, 2020
Export Citation:
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Assignee:
LUOXIN PHARMACEUTICAL SHANGHAI CO LTD (CN)
SHANDONG LUOXIN PHARMACY STOCK (CN)
International Classes:
C07D309/10; A61K31/351; A61P3/10
Domestic Patent References:
WO2016018024A12016-02-04
WO2017202264A12017-11-30
WO2018029611A12018-02-15
WO2016155578A12016-10-06
WO2017046730A12017-03-23
WO2017118945A12017-07-13
Foreign References:
CN107163092A2017-09-15
CN108084130A2018-05-29
CN101479287A2009-07-08
Attorney, Agent or Firm:
SHANGHAI BESHINING LAW OFFICE (CN)
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