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Dabigatran etexilate mesylate solid pharmaceutical preparation and preparation method thereof

A technology for dabigatran etexilate mesylate and solid pharmaceutical preparations, which is applied in the field of dabigatran etexilate mesylate solid pharmaceutical preparations and their preparation, can solve the problem that the requirements for parameter control are quite high, the non-compliance with green chemistry, and the production process Complex problems, etc., to achieve the effect of simple and controllable preparation method, saving tartaric acid auxiliary materials, and high production feasibility

Inactive Publication Date: 2020-05-15
南京嘉晨医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This process has very high requirements for parameter control in the production process. In addition, there are some problems in continuous production. The production process is complicated and the production cycle is long, which is not conducive to large-scale industrial production. The weight ratio of ketone esters is 1:1, and the amount of tartaric acid is relatively large, which does not meet the requirements of green chemistry

Method used

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  • Dabigatran etexilate mesylate solid pharmaceutical preparation and preparation method thereof
  • Dabigatran etexilate mesylate solid pharmaceutical preparation and preparation method thereof
  • Dabigatran etexilate mesylate solid pharmaceutical preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041]

[0042]

[0043] (1) The raw material drug dabigatran etexilate mesylate is micronized, the feed rate is set to be 10g / min, the feed pressure is 0.7-0.9MPa, and the crushing pressure is 0.6-0.8MPa; the final particle size of the control raw material The diameter is d50=3.17 μm, d90=4.83 μm.

[0044] (2) Weigh the prescribed amount of simethicone and add it to ethanol, then disperse and dissolve the prescribed amount of hydroxypropyl methylcellulose into the ethanol, and finally disperse the talcum powder into the above liquid, and keep stirring for 45 minutes to obtain the isolation layer coating liquid.

[0045] (3) Dissolve the prescribed amount of hydroxypropyl cellulose in isopropanol, then evenly disperse the prescribed amount of dabigatran etexilate into the above-mentioned liquid, finally add talcum powder therein, keep stirring for 45min, and 100-mesh sieve for subsequent use to obtain the drug-containing layer coating solution.

[0046] (4) Weigh the p...

Embodiment 2

[0050]

[0051] The weight of each component in embodiment 2 is according to the data in the table above, and the preparation steps are the same as in embodiment 1.

Embodiment 3

[0053]

[0054]

[0055] (1) The raw material drug dabigatran etexilate mesylate is micronized, the feed rate is set to be 10g / min, the feed pressure is 0.7-0.9MPa, and the crushing pressure is 0.6-0.8MPa; the final particle size of the control raw material The diameter is d50=4.86 μm, d90=9.27 μm.

[0056] All the other processing steps are with embodiment 1.

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Abstract

The invention provides a dabigatran etexilate mesylate solid pharmaceutical preparation and a preparation method thereof, and belongs to the field of pharmaceutical preparations. In the present invention, a fluidized bed bottom-spraying coating process is used to sequentially coat an isolation layer containing talcum powder, hydroxypropyl methylcellulose and dimethicone, and a drug-containing layer containing dabigatran etexilate mesylateactive ingredientson surface of tartaric acidpellets to obtain drug-containing pellets, and then the drug-containing pellets are encapsulated in capsules. Theresulting dabigatran etexilate mesylate solid pharmaceutical preparation has more than 95% of dissolution rate within 30 min and improved dissolution rate. The drug-containing pellets are uniform inweight and good in stability, higher in roundness and narrower in particle size distribution. Meanwhile, the preparation method is simple and controllable, saves tartaric acid auxiliary materials andimproves feasibility of industrial production.

Description

technical field [0001] The invention relates to a solid pharmaceutical preparation of dabigatran etexilate mesylate and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Dabigatran etexilate mesylate is the mesylate of dabigatran etexilate, and its structural formula is as follows: [0003] [0004] Dabigatran etexilate mesylate was researched and developed by Boehringer Ingelheim (Boehringer Ingelheim) in Germany. It is a new type of oral anticoagulant and belongs to non-peptide thrombin inhibitors. In April 2008, it was first launched in Germany and the United Kingdom under the trade name of Pradaxa. It is the first new class of oral anticoagulant drug to be launched in the past 50 years after warfarin. It is approved in the European Union for total hip or total knee replacement surgery Prevention of posterior venous thrombosis. After oral administration, the drug releases dabigatran in the body, binds t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/4439A61P7/02A61K9/50
CPCA61K9/485A61K9/5078A61K31/4439A61P7/02
Inventor 杨勇
Owner 南京嘉晨医药科技有限公司
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