Title:
EUTECTIC CRYSTAL FORMED BY APIXABAN AND CARBOXYLIC ACID, AND PREPARATION METHOD THEREFOR
Document Type and Number:
WIPO Patent Application WO/2021/056850
Kind Code:
A1
Abstract:
Provided are an eutectic crystal formed by apixaban and a carboxylic acid, and a preparation method therefor. The eutectic crystal comprises an apixaban/malonic acid eutectic crystal, an apixaban/D‐malate eutectic crystal, an apixaban/maleic acid eutectic crystal, an apixaban/L‐proline eutectic crystal, and an apixaban/L‐tartaric acid eutectic crystal. The eutectic crystal solves the disadvantages of a slow dissolution rate and a low dissolution rate of apixaban, has an improved dissolution rate of apixaban, and is beneficial to improve bioavailability.
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Inventors:
ZHU GUORONG (CN)
KE CHUNLONG (CN)
WANG ZHEN (CN)
TU YONGJUN (CN)
ZHANG PENG (CN)
KE CHUNLONG (CN)
WANG ZHEN (CN)
TU YONGJUN (CN)
ZHANG PENG (CN)
Application Number:
PCT/CN2019/125115
Publication Date:
April 01, 2021
Filing Date:
December 13, 2019
Export Citation:
Assignee:
ZHEJIANG TIANYU PHARMACEUTICAL CO LTD (CN)
International Classes:
C07D471/04; C07C51/43; C07C55/08; C07C57/02; C07C59/255; C07D207/16
Domestic Patent References:
| WO2012168364A1 | 2012-12-13 |
Foreign References:
| CN110452240A | 2019-11-15 | |||
| CN106986868A | 2017-07-28 | |||
| CN105985336A | 2016-10-05 | |||
| CN104370902A | 2015-02-25 | |||
| CN105175415A | 2015-12-23 | |||
| CN104797580A | 2015-07-22 | |||
| US20070203178A1 | 2007-08-30 | |||
| CN101065379A | 2007-10-31 | |||
| US20070203178A1 | 2007-08-30 | |||
| CN104086544A | 2014-10-08 | |||
| CN106986868A | 2017-07-28 | |||
| CN101065379A | 2007-10-31 |
Other References:
LARKIN, PETER J. ET AL.: "Polymorph Characterization of Active Pharmaceutical Ingredients (APIs) Using Low-Frequency Raman Spectroscopy.", APPLIED SPECTROSCOPY, vol. 68, no. 7, 1 July 2014 (2014-07-01), XP055795762, ISSN: 0003-7028
CHEN YONG, LI LONG, YAO JIA, MA YU-YU, CHEN JIA-MEI, LU TONG-BU: "Improving the Solubility and Bioavailability of Apixaban via Apixaban–Oxalic Acid Cocrystal", CRYSTAL GROWTH & DESIGN, ASC WASHINGTON DC, US, vol. 16, no. 5, 4 May 2016 (2016-05-04), US, pages 2923 - 2930, XP055795763, ISSN: 1528-7483, DOI: 10.1021/acs.cgd.6b00266
See also references of EP 3932918A4
CHEN YONG, LI LONG, YAO JIA, MA YU-YU, CHEN JIA-MEI, LU TONG-BU: "Improving the Solubility and Bioavailability of Apixaban via Apixaban–Oxalic Acid Cocrystal", CRYSTAL GROWTH & DESIGN, ASC WASHINGTON DC, US, vol. 16, no. 5, 4 May 2016 (2016-05-04), US, pages 2923 - 2930, XP055795763, ISSN: 1528-7483, DOI: 10.1021/acs.cgd.6b00266
See also references of EP 3932918A4
Attorney, Agent or Firm:
SINO-CREATIVITY INTELLECTUAL PROPERTY LAW FIRM (CN)
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