Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Stable dabigatran etexilate mesylate compound

A technology of dabigatran etexilate mesylate and methanesulfonic acid, applied in the field of medicine, can solve the problems of high impurities, moisture absorption and weight gain, etc.

Inactive Publication Date: 2015-03-25
TIANJIN HANKANG PHARMA BIOTECH
View PDF3 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The production method impurity of above-mentioned dabigatran etexilate mesylate is higher, also has certain hygroscopic weight gain

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Stable dabigatran etexilate mesylate compound
  • Stable dabigatran etexilate mesylate compound
  • Stable dabigatran etexilate mesylate compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The dabigatran etexilate of 20g is dissolved in by 50ml acetone, in the mixture that the ethyl acetate of 80ml and 50ml diisopropyl ether form, add the water of 2ml, then to wherein dropwise the methanesulfonic acid of 6.5g, reaction mixture Stir for 2.5 hours, cool to 12°C, filter, wash the filtered crystals with 40ml of isopropyl acetate and 40ml of isopropyl ether, and filter and dry at room temperature to obtain 25.7g of Dabiga methanesulfonate Group ester crystals, the content is 99.86%, and the single impurity is less than 0.08%. Determined by Karl Fischer method, it contains 2.43% (weight percent) of water.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

Belongs to the technical field of medicines, the invention in particular relates to a hydrate of dabigatran etexilate mesylate and a preparation method thereof. The hydrate of dabigatran etexilate mesylate obtained by the invention contains a crystal water, and has the advantages of high purity, good stability, and non-obvious moisture absorption weight gain even under a high humidity condition.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to dabigatran etexilate methanesulfonate hydrate and a preparation method thereof, and the invention also relates to a composition using the hydrate for reducing stroke and systemic embolism in patients with non-valvular atrial fibrillation risky application. Background technique [0002] Dabigatran etexilate is a new type of synthetic direct thrombin inhibitor, which is the prodrug of dabigatran and is a non-peptide thrombin inhibitor. After oral administration and gastrointestinal absorption, it is transformed into dabigatran with direct anticoagulant activity in vivo. Dabigatran binds to the fibrin-specific binding site of thrombin, preventing fibrinogen from being cleaved into fibrin, thereby blocking the final step of the coagulation cascade network and thrombus formation. Dabigatran dissociates from the fibrin-thrombin complex and exerts a reversible anticoagulant effect. ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07D401/12C07C309/04C07C303/32A61K31/4439A61P9/10A61P7/02
CPCC07D401/12
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com