Dabigatran etexilate mesylate oral solid preparation and preparation method thereof

A technology for dabigatran etexilate mesylate and dabigatran etexilate, which is applied in the directions of pill delivery, pharmaceutical formulation, coating, etc. The effect of reducing coating steps and simplifying the production process

Inactive Publication Date: 2016-05-04
郑州大明药物科技有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method isolates the drug from the organic acid by coating the core of the drug pellet, but during the tableting process, the isolation film on the core of the drug pellet may be broken, allowing the drug to come into contact with the organic acid, reducing the stability of the drug

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 prescription and preparation process

[0032]

[0033] Preparation:

[0034] 1) Weigh the main drug and various auxiliary materials required for the prescription, and pass the main drug through a 100-mesh sieve for use;

[0035] 2) Take a prescription amount of polyethylene glycol and heat it to 50~60℃ to make it into a molten liquid;

[0036] 3) Under slow stirring, add the prescription amount of dabigatran etexilate mesylate and 40% of the prescription amount of disintegrant in batches. After the addition is complete, stir slowly for 15~30min, and stir vigorously for 30~60min to disintegrate the drug. The solution is evenly dispersed. The speed of slow stirring is 150~300 rpm, and the speed of vigorous stirring is 5000~10000 rpm;

[0037] 4) Place the molten liquid prepared in step 3) under -20°C and rapidly cool down and solidify for 2~3 hours to obtain a solidified product;

[0038] 5) The solidified product obtained in step 4) is crushed at 5~10°C, passed through ...

Embodiment 2

[0043] Embodiment 2 prescription and preparation process

[0044] .

Embodiment 3

[0045] Example 3 Recipe and preparation process

[0046] .

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PUM

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Abstract

The invention provides a dabigatran etexilate mesylate oral solid preparation. With a specification of 110mg (based on free dabigatran etexilate), each tablet of the dabigatran etexilate mesylate oral solid preparation comprises the following components: 127mg of dabigatran etexilate mesylate (110mg of dabigatran etexilate), 180-190mg of water-soluble polymer, 15-20mg of disintegrant and 3.0-5.0mg of lubricant. According to the solid medicinal preparation provided by the invention, main drugs are dispersed in a water-soluble carrier, thus the dissolution rate of the preparation is increased, and the drug content uniformity is guaranteed. The dabigatran etexilate mesylate oral solid preparation provided by the invention is simple in preparation technology and suitable for industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a solid pharmaceutical preparation containing dabigatran etexilate mesylate and a preparation method thereof. Background technique [0002] The chemical name of dabigatran etexilate mesylate (Dabigatranetexilatemesylate) [0003] 3-[(2-{[4-(Hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridine- 2-yl-amino]-propionic acid ethyl ester methanesulfonate, formula C 34 h 41 N 7 o 5 CH 4 o 3 S, relative molecular mass 723.84. Dabigatran etexilate mesylate is a new type of non-peptide direct thrombin inhibitor, which was approved by the US FDA on October 19, 2010 for the prevention of stroke and systemic embolism in patients with non-valvular atrial fibrillation treat. Dabigatran etexilate mesylate has the characteristics of oral administration, strong potency, no need for special drug monitoring, and few drug interacti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/30A61K31/4439A61K47/34A61K47/38A61P7/02A61P9/10
CPCA61K9/2031A61K9/2054A61K9/2813A61K9/2853A61K9/2866A61K31/4439
Inventor 刘志庆樊振吕和平毛影李沁沁朱赞梅
Owner 郑州大明药物科技有限公司
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