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Pharmaceutical composition containing dabigatran etexilate or salt and hydrate thereof

A hydrate and composition technology, applied in the field of medicine, can solve the problems of low yield of finished products, small dosage of medicine, difficult to control dosage of medicine, etc., and achieve good storage stability, good dissolution and dissolution, and bioavailability effect. outstanding effect

Active Publication Date: 2013-06-05
NANJING HUAWE MEDICINE TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The dosage of this method is small, and it is difficult to control the dosage of the drug, the drug layer is uneven, the reproducibility between batches is poor, the loss of raw materials is large, and the yield of finished products is low.

Method used

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  • Pharmaceutical composition containing dabigatran etexilate or salt and hydrate thereof
  • Pharmaceutical composition containing dabigatran etexilate or salt and hydrate thereof
  • Pharmaceutical composition containing dabigatran etexilate or salt and hydrate thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1 preparation of pellet core material containing active substance

[0034] Example

active substance

lactose

Polyvinylpyrrolidone

2-propanol

1

20

20

4

36

[0035] Weighing 4g wrong! Reference source not found. Dissolved in 36 g of 2-propanol. Mix 20g of dabigatran etexilate mesylate (active substance) and 20g of lactose with mechanical stirring, then add 4g of wrong! Reference source not found. A solution of 2-propanol (36g) was mixed into a suitable soft material and passed through an extrusion spheronizer to form roughly spherical particles. Then the spherical active material core material is dried on a fluidized bed at a material temperature of 30-35° C. to obtain active material ball cores.

[0036] The core material was separated using a drum screener with perforated plates of nominal mesh size 0.6-1.0 mm. The product fraction between 0.6-1.0 mm was used in the remainder of the process.

Embodiment 2-10

[0037] Embodiment 2-10 preparation of active substance ball core material

[0038]

[0039]

[0040] Examples 2-10 Active substance pellet core materials were prepared in the same manner as in Example 1.

Embodiment 11-17

[0041] The preparation of embodiment 11-17 active substance ball core material

[0042]

[0043] Examples 11-17 Active substance pellet core materials were prepared in the same manner as in Example 1.

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Abstract

The invention discloses a pharmaceutical composition containing dabigatran etexilate or salt and hydrate of the dabigatran etexilate. The pharmaceutical composition comprises an active substance pill core material containing the dabigatran etexilate or its pharmaceutically acceptable salt or hydrate and a filling agent and / or a bonding agent,and an organic acid or an organic acid material layer, the organic acid is arranged outside the active substance pill core materials, the organic acid material layer contains the organic acid, and the organic acid is selected from tartaric acid, succinic acid, citric acid, glutamic acid, fumaric acid, malic acid, aspartic acid or their hydrates or salts. After screening, the dabigatran etexilate active substance is prepared into a pill core, the organic acid material layer is added in an integrated mode, and meanwhile, an isolated layer is applied between the dabigatran etexilate active substance pill core and the organic acid material layer. The prepared dabigatran etexilate oral drugs composition has the advantages that solubility and dissolution rate are good, and bioavailability effect is prominent.

Description

technical field [0001] The invention relates to a pharmaceutical composition of active substance dabigatran etexilate and pharmacologically acceptable salts and hydrates thereof, belonging to the technical field of medicines. Background technique [0002] The chemical name of the dabigatran etexilate active substance of the present invention is 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1- Methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester and its salts and hydrates. The chemical structure of dabigatran etexilate is shown in the following scheme I. It is a new type of synthetic non-peptide thrombin inhibitor, which is the prodrug of dabigatran (dabigatran), and is mainly used for the prevention of venous thrombosis after surgery. After oral administration, dabigatran etexilate is converted into dabigatran with direct anticoagulant activity after gastrointestinal absorption. Dabigatran binds to the fibrin-specific bi...

Claims

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Application Information

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IPC IPC(8): A61K31/4439A61K9/48A61P7/02
Inventor 张孝清许瑞包金远程晓佳蒋玉伟
Owner NANJING HUAWE MEDICINE TECH DEV
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