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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
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  • 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

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  • 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.

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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

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Application Information

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IPC IPC(8): C07D401/12C07C309/04C07C303/32A61K31/4439A61P9/10A61P7/02
CPCC07D401/12
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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