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Pharmaceutical preparation of dabigatran etexilate mesylate

A technology for dabigatran etexilate mesylate and a pharmaceutical preparation, which is applied in the field of pharmaceutical preparations of direct thrombin inhibitors, can solve problems such as poor stability, and achieve the effects of ensuring curative effect, good dissolution effect, good dissolution and stability

Active Publication Date: 2021-11-02
BEIJING WINSUNNY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But dabigatran etexilate mesylate is not stable in acidic environment, if encounter moisture in acidic environment, its stability is worse

Method used

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  • Pharmaceutical preparation of dabigatran etexilate mesylate
  • Pharmaceutical preparation of dabigatran etexilate mesylate
  • Pharmaceutical preparation of dabigatran etexilate mesylate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042]

[0043]

[0044] Preparation:

[0045] (1) Dabigatran etexilate mesylate, lactose, xanthan gum and guar gum are dispersed in water, spray drying makes dabigatran etexilate mesylate complex, in dabigatran etexilate mesylate The surface of the compound is coated with an isolation coat to obtain the dabigatran etexilate mesylate coating compound, and the dabigatran etexilate mesylate coating compound particle diameter d0.9 is 300 μm;

[0046] (2) The dabigatran etexilate mesylate coating compound was mixed with tartaric acid, and filled into capsules.

Embodiment 2

[0048]

[0049] Preparation:

[0050] (1) dabigatran etexilate mesylate, mannitol, xanthan gum and guar gum are dispersed in 30% ethanol aqueous solution, spray drying makes dabigatran etexilate mesylate complex, in methanesulfonic acid The surface of the dabigatran etexilate complex is coated with an isolation coat to obtain the dabigatran etexilate mesylate coating complex, and the dabigatran etexilate mesylate coating complex particle diameter d0.9 is 250 μm;

[0051] (2) The dabigatran etexilate mesylate coating complex and fumaric acid were mixed, and filled into capsules.

Embodiment 3

[0053]

[0054]

[0055] Preparation:

[0056] (1) Dabigatran etexilate mesylate, lactose, sucrose, xanthan gum, guar gum and sodium lauryl sulfate are dispersed in methylene chloride, and spray drying makes dabigatran etexilate mesylate Composite, coat isolation coat on the surface of dabigatran etexilate mesylate complex, obtain dabigatran etexilate mesylate coating complex, dabigatran etexilate mesylate coating complex particle size d0.9 460μm;

[0057] (2) The dabigatran etexilate mesylate coating compound was mixed with succinic acid, and filled into capsules.

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Abstract

The present invention relates to a dabigatran etexilate mesylate pharmaceutical preparation. The pharmaceutical preparation specifically comprises a dabigatran etexilate mesylate coating compound and an organic acid or a dabigatran etexilate mesylate compound and organic acid-containing coating particles, wherein the compound comprises dabigatran etexilate mesylate, a water-soluble diluent and a glue material; and the gum material is one or more of xanthan gum, guar gum, locust bean gum and carrageenan. The dabigatran etexilate mesylate pharmaceutical preparation prepared by the invention has better dissolution rate and stability, and the preparation method is simple, easy to operate and suitable for industrial large-scale production.

Description

technical field [0001] The invention relates to a pharmaceutical preparation of a direct thrombin inhibitor, in particular to a pharmaceutical preparation of dabigatran etexilate mesylate, and a preparation method of the preparation. Background technique [0002] Atrial fibrillation (AF) is the most common arrhythmia disease clinically. The investigation shows that the prevalence of atrial fibrillation in my country is as high as 0.77%, and the prevalence shows a trend of increasing significantly with age. With the increasingly prominent problem of population aging in my country, the prevalence of atrial fibrillation will continue to increase. Cardiogenic stroke (mainly ischemic stroke) is the most serious complication of atrial fibrillation, with a high rate of death and disability. Therefore, stroke prevention is very important for patients with atrial fibrillation. The basis of stroke prevention is anticoagulant therapy. Warfarin is the oral anticoagulant drug with the m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61K9/48A61K9/50A61K47/36A61K47/26A61K47/12A61K47/18A61K9/16A61P7/02A61P9/10
CPCA61K31/4439A61K9/4808A61K9/4866A61K9/4858A61K9/4833A61K9/5047A61K9/5089A61K47/36A61K47/26A61K9/1652A61K9/1623A61P7/02A61P9/10Y02A50/30
Inventor 黄玉锋杨文涛彭小玲吕海东
Owner BEIJING WINSUNNY PHARMA CO LTD
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