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Title:
COCRYSTAL OF DABIGATRAN ETEXILATE AND METHOD FOR PREPARING SAME
Document Type and Number:
WIPO Patent Application WO/2023/174090
Kind Code:
A1
Abstract:
The present invention relates to a cocrystal of dabigatran etexilate and a method for preparing same, also relates to a pharmaceutical composition comprising the cocrystal, and further relates to use of the cocrystal in preparing an anticoagulant drug. The cocrystal comprises dabigatran etexilate and a cocrystal former, the cocrystal former being a specific type of organic acid. The cocrystal has the advantages of high solubility, high in vitro dissolution rate, high in vivo relative bioavailability, and the like.

Inventors:
JIN HAIMING (CN)
Application Number:
PCT/CN2023/079856
Publication Date:
September 21, 2023
Filing Date:
March 06, 2023
Export Citation:
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Assignee:
QINGDAO HUAQI PHARMACEUTICAL TECH INNOVATION DEVELOPMENT CO LTD (CN)
International Classes:
C07D401/12; A61K31/4439; A61P7/02
Domestic Patent References:
WO2019008605A12019-01-10
WO2014020546A22014-02-06
WO2013124749A12013-08-29
Foreign References:
EP2610251A12013-07-03
US20170165247A12017-06-15
Other References:
GAWADE A R, BOLDHANE S P: "SOLID DOSAGE FORM DEVELOPMENT OF DABIGATRAN ETEXILATE MESYLATE WITH INCREASED SOLUBILITY AND DISSOLUTION USING COCRYSTALLIZATION", INTERNALTIONAL JOURNAL OF PHARMACEUTICAL SCIENCES AND RESEARCH, SOCIETY OF PHARMACEUTICAL SCIENCES AND RESEARCH, PNACHKULA (HR), IN, vol. 11, no. 6, 1 June 2020 (2020-06-01), IN , XP093092654, ISSN: 2320-5148, DOI: 10.13040/IJPSR.0975-8232.11(5).2899-05
ZHANG, XIAOMING: "Pharmaceutical Co-crystal Synthesis, Representation and Property Research", CHINA DOCTORAL DISSERTATIONS FULL-TEXT DATABASE, ENGINEERING SCIENCE AND TECHNOLOGY 1, 15 August 2016 (2016-08-15), pages B014 - 91, ISSN: 1674-022X
"Pharmaceutics", 30 April 2020, CHINA MEDICAL SCIENCE AND TECHNOLOGY PRESS, CN, ISBN: 978-7-5214-1761-6, article QI, XIAOLE: "XI. Pharmaceutical Co- crystal Technology", pages: 379 - 381, XP009549916
Attorney, Agent or Firm:
CCPIT PATENT AND TRADEMARK LAW OFFICE (CN)
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