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A kind of dabigatran etexilate tablet and preparation method thereof

A technology for dabigatran etexilate and gatran etexilate tablets, applied in the field of dabigatran etexilate tablets and its preparation, can solve the problems of high requirements, cumbersome operations, damage to the gastrointestinal tract, etc., and reduce production costs , reduce irritation and damage, and achieve the effect of industrialization

Active Publication Date: 2019-01-18
LIANGJIANG MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This process not only has high requirements on acid-containing core materials, but also needs crystals or nearly spherical particles with a certain diameter, and the operation is cumbersome.
Most importantly, in the capsules disclosed in the above-mentioned patents, after the organic acid is released with the drug, it is easy to form a local low pH environment and damage the gastrointestinal tract.

Method used

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  • A kind of dabigatran etexilate tablet and preparation method thereof
  • A kind of dabigatran etexilate tablet and preparation method thereof
  • A kind of dabigatran etexilate tablet and preparation method thereof

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Effect test

preparation example Construction

[0071] The present invention also provides a kind of preparation method of dabigatran etexilate tablet, comprising:

[0072] A) uniformly mixing the organic acid and the sustained-release material and dry granulating to obtain organic acid granules;

[0073] B) mixing dabigatran etexilate and pharmaceutically acceptable salts thereof and auxiliary materials and dry granulating to obtain dabigatran etexilate granules;

[0074] C) the organic acid granules and the dabigatran etexilate granules are compressed by a double-layer tablet press to obtain a double-layer tablet; or by a three-layer tablet press, the middle layer is the dabigatran etexilate layer, and the other two The first layer is an organic acid layer to obtain a three-layer tablet; or the tablet is compressed by a three-layer tablet machine, the middle layer is an auxiliary material layer, and the remaining two layers are respectively an organic acid layer and a dabigatran etexilate layer to obtain a three-layer tab...

Embodiment 1

[0083] According to the ingredients listed in Table 1, the components of dabigatran etexilate and organic acid were made into granules by dry granulation, and then compressed into double-layer tablets, and then Opadry II film-coated premix was used The coating material is used for coating.

[0084] Table 1 embodiment 1 group distribution ratio

[0085]

Embodiment 2

[0087] According to the ingredients listed in Table 2, the components of dabigatran etexilate and organic acid were made into granules by dry granulation, and then compressed into double-layer tablets.

[0088] Table 2 Example 2 group distribution ratio

[0089]

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Abstract

The present invention provides a dabigatran tablet, including a dabigatran layer, an organic acid layer compounded on the surface of the dabigatran layer. The organic acid layer includes organic acid and a sustained-release material; the organic acid is citric acid or tartaric acid; the sustained-release material is one or more of hydroxypropyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, ethyl cellulose and hydroxyethyl cellulose; the dabigatran layer includes dabigatran and a pharmaceutically acceptable salt thereof; the content of the organic acid is 20wt%-50wt%; and the content of the slow release material is 5wt%-20wt%. The organic acid in the dabigatran tablet can release at a constant speed or slowly, thereby reducing the stimulation and injury of gastrointestinal drugs, but does not affect the bioavailability of the drug. At the same time, the preparation method is more simple and easy to operate, reduces the production cost, and is easy to realize industrialization.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a dabigatran etexilate tablet and a preparation method thereof. Background technique [0002] Dabigatran etexilate, as shown in compound I, is a newly synthesized direct thrombin inhibitor, a prodrug of dabigatran, and a non-peptide thrombin inhibitor. After oral administration and gastrointestinal absorption, it is transformed into dabigatran with direct anticoagulant activity in the body. 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. [0003] [0004] The absolute bioavailability of dabigatran etexilate after oral administration is 3% to 7%, and the blood drug concentration reaches the peak ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/24A61K9/36A61K31/4439A61K47/12A61K47/38A61P7/02
CPCA61K9/2013A61K9/2054A61K9/2086A61K9/209A61K9/2866A61K31/4439
Inventor 赵小萍肖娟黄晓宇李秋静陈海军贺耘
Owner LIANGJIANG MEDICINE CO LTD
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