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High-bioavailability dabigatran etexilate pharmaceutical composition

A technology for dabigatran etexilate and dabigatran etexilate mesylate, which is applied in the field of high bioavailability dabigatran etexilate pharmaceutical compositions, can solve problems such as gastrointestinal adverse reactions, and achieve gastric protection. Intestinal mucosa, reducing the risk of recurrence, and improving the effect of bioavailability

Inactive Publication Date: 2017-06-27
BEIJING LANDAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In addition to absorption problems, another problem in the clinical use of dabigatran etexilate is gastrointestinal adverse reactions

Method used

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  • High-bioavailability dabigatran etexilate pharmaceutical composition
  • High-bioavailability dabigatran etexilate pharmaceutical composition
  • High-bioavailability dabigatran etexilate pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 dabigatran etexilate mesylate, betaine hydrochloride pellet capsule

[0029]

[0030] According to the prescription in the above table, adopt the method of patent CN101632668A embodiment 1 to prepare dabigatran etexilate mesylate betaine hydrochloride pellets (replace tartaric acid in the method with betaine hydrochloride).

[0031] The micropills can be packed into capsules or directly packed, and the clinical dosage is 75 mg to 300 mg based on dabigatran etexilate, so as to adjust different loading amounts. For example, each dosage can be 75 mg of dabigatran etexilate (the corresponding amount of betaine hydrochloride is 750 mg), and 150 mg of dabigatran etexilate (the corresponding amount of betaine hydrochloride is 1500 mg).

Embodiment 2

[0060] Embodiment 2 dabigatran etexilate mesylate, betaine citrate pellet capsule

[0061] Element Dosage / g use Dabigatran etexilate mesylate 57.7 (equivalent to dabigatran etexilate 50g) active ingredient betaine citrate 200 active ingredient microcrystalline cellulose 100 filler Micropowder silica gel 10 lubricant Hydroxypropyl Cellulose 35 Adhesive

[0062] 1. Preparation of betaine citrate pellet core

[0063] Take the prescription amount of betaine citrate, pulverize and sieve; take microcrystalline cellulose and pass it through an 80-mesh sieve; mix betaine hydrochloride and microcrystalline cellulose evenly, add water to prepare soft material, and make pellets by extrusion spheronization, and dry.

[0064] 2. Pack isolation gown

[0065] The betaine hydrochloride pellets prepared in step 1 were placed in a fluidized bed, and a 3% HMPC aqueous solution was used as a coating solution for bottom spray coating, and...

Embodiment 3

[0070] Embodiment 3 dabigatran etexilate mesylate, betaine hydrochloride compression-coated tablet

[0071] Prescription (1000 tablets):

[0072] Tablet composition Dosage / g Dabigatran etexilate mesylate 86.5 (equivalent to dabigatran etexilate 75g) lactose monohydrate 80 microcrystalline cellulose 55.5 Magnesium stearate 3.5 Polyvinylpyrrolidone 4.5

[0073] Preparation Process:

[0074] (1) Mix dabigatran etexilate mesylate, lactose monohydrate and microcrystalline cellulose evenly.

[0075] (2) Make polyvinylpyrrolidone into 10% ethanol solution of polyvinylpyrrolidone as an adhesive.

[0076] (3) Add the 10% polyvinylpyrrolidone ethanol solution prepared in the step (2) to the step (1) to make a soft material.

[0077] (4) Pass the soft material prepared in step (3) through a 20-mesh sieve for wet granulation.

[0078] (5) Dry the granules prepared in step (4) at 60° C. for 0.5 h.

[0079] (6) Pass the granules in step (5...

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Abstract

The invention provides a high-bioavailability dabigatran etexilate pharmaceutical composition. The pharmaceutical composition comprises the following two components in parts by weight: 50-400 parts of dabigatran etexilate and salt thereof, and 200-2000 parts of betaine and salt thereof. The dabigatran etexilate pharmaceutical composition provided by the invention can increase the dabigatran etexilate bioavailability, and also can relieve the untoward reaction of the gastrointestinal tract in the use process.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a pharmaceutical composition of dabigatran etexilate with high bioavailability. Background technique [0002] Dabigatran etexilate is a new type of synthetic direct thrombin inhibitor, which is the prodrug of dabigatran and belongs to non-peptide thrombin inhibitors. The structural formulas of dabigatran etexilate and dabigatran are as follows: [0003] [0004] In April 2008, dabigatran etexilate was first listed in Germany and the United Kingdom, and then it was approved for listing and widely used in more than 40 countries. It was approved by the US FDA in 2010. In 2013, dabigatran etexilate was approved by CFDA for import. Dabigatran etexilate is rapidly absorbed orally, and is rapidly converted into dabigatran with direct anticoagulant activity by non-specific esterase-catalyzed hydrolysis in the body. The oral absolute bioavailability of dabigatran etexilate is 3-7%...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61K31/205A61P7/02
CPCA61K31/4439A61K9/1652A61K31/205A61K2300/00
Inventor 林静文其他发明人请求不公开姓名
Owner BEIJING LANDAN PHARMA TECH
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