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Pharmaceutical composition containing pradaxa mesylate and preparation method thereof

A technology of dabigatran etexilate mesylate and composition, which is applied in the field of pharmaceutical composition containing dabigatran etexilate mesylate and its preparation, and can solve the problem of crystal form transformation of active substances, complex process, and environmental problems. pollution and other issues

Active Publication Date: 2015-08-12
SEASONS BIOTECHNOLOGY (TAIZHOU) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Through repeated experiments by the inventors, it was found that the use of organic solvents, in addition to the aforementioned problems such as complicated process, increased cost, and environmental pollution, would also cause crystal transformation of the active substance, thereby affecting the stability and dissolution rate of the preparation.

Method used

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  • Pharmaceutical composition containing pradaxa mesylate and preparation method thereof
  • Pharmaceutical composition containing pradaxa mesylate and preparation method thereof
  • Pharmaceutical composition containing pradaxa mesylate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example

[0074] The starting material dabigatran etexilate mesylate form I can be prepared according to the method disclosed in Example 1 of WO2005028468A1.

[0075] The specific operation is: add 293 grams of acetone to 52.6 grams of dabigatran etexilate, and heat to 42° C. under stirring to form a clear solution. Afterwards, filter into a second stirring device followed by cooling to 33°C. Prepare 33 grams of acetone at 2° C., 7.9 grams of 99.5% methanesulfonic acid and 9 grams of acetone for rinsing, at 30° C. within 25 minutes, add to the solution of dabigatran etexilate with distribution metering, mixture 30 ℃ for 60 minutes, then cooled to 20 ℃ and stirred for 60 minutes. The crystal suspension was filtered, washed with 270 mL of acetone, and dried in vacuum at a maximum temperature of 50° C. for at least 4 hours to obtain crystalline form I of dabigatran etexilate mesylate.

Embodiment 1

[0077] According to the preparation method of the present invention, the pharmaceutical composition of the present invention using dabigatran etexilate methanesulfonate crystal form I as the active substance is prepared, and the formula and preparation method of each step are as follows.

[0078] (1) Preparation of Active Material Ball Core

[0079]

[0080] The preparation method of the active substance pellet core of No. 1a: Weigh 5g of hydroxypropyl methylcellulose, slowly add it into 20g of 80°C purified water under stirring, let it stand and cool to room temperature, dissolve the hydroxypropylmethylcellulose, and prepare into a binder solution. Put 85g of dabigatran etexilate mesylate mesylate crystal form I and 10g of microcrystalline cellulose into a wet granulator, mix well, and then add the above-mentioned prepared binder solution to make a suitable soft material. The soft material is extruded through a 0.6mm sieve and then rounded to obtain roughly spherical part...

Embodiment 2

[0102] (1) Preparation of active material ball core:

[0103] components

Weight (g)

Dabigatran etexilate mesylate crystal form I

70

microcrystalline cellulose

25

Hydroxypropylmethylcellulose

5

purified water

10

Total (dry weight)

100

[0104] Weigh 5g of hydroxypropylmethylcellulose, slowly add it into 10g of 80°C purified water with stirring, let it stand and cool to room temperature, dissolve the hydroxypropylmethylcellulose, and prepare a binder solution. Put 70g of dabigatran etexilate methanesulfonate crystal form I and 25g of microcrystalline cellulose into a wet granulator, mix well, and then add the above-mentioned prepared binder solution to make a suitable soft material. The soft material is granulated through a 20-mesh sieve, and the prepared granules are dried in a fluidized bed at a material temperature of 30-35°C for 8-10 hours until the moisture content of the granules is less than 1%, ...

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Abstract

The invention relates to a pharmaceutical composition containing pradaxa mesylate and a preparation method thereof. Compared with prior art, the preparation method has the advantages of simple process, low production cost and environmental protection. The obtained pharmaceutical composition has the advantages of stable crystal form of active substance, good storage stability and high dissolvability.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a pharmaceutical composition containing dabigatran etexilate mesylate and a preparation method thereof. Background technique [0002] Dabigatran (dabigatran), developed by Boehringer Ingelheim (Boehringer Ingelheim) in Germany, is a new type of oral anticoagulant, which belongs to non-peptide thrombin inhibitors, and is mainly used for the prevention of deep vein thrombosis after surgery. . The drug was first launched in Germany and the UK in April 2008, and was approved by the FDA in 2010 to reduce the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation. The drug has the advantages of oral administration, strong potency, no need for special medication monitoring, and few drug interactions. [0003] The chemical name of dabigatran is N-[[2-[[[4-(aminoiminomethyl)phenyl]amino]methyl]-1-methyl-1H-benzo[D]imidazole-5 -yl]carbonyl]-N-pyridin-2-y...

Claims

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Application Information

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IPC IPC(8): A61K9/62A61K9/26A61K31/4439A61P7/02
Inventor 贾强杨晓玲
Owner SEASONS BIOTECHNOLOGY (TAIZHOU) CO LTD
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