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Dispersion preparation containing dabigatran etexilate

A technology of dabigatran etexilate and dispersant, applied in the field of medicine, can solve the problems of complex operation process, complex process operation, uneven drug application and the like

Inactive Publication Date: 2014-03-19
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The process applies the drug by fluidizing the surface of the organic acid pill core, that is, the drug is configured into a suspension for drug application. This method has the advantages of low drug application rate, large drug loss, complicated process operation, uneven drug application, and high drug dosage. Uncertainty and other shortcomings; due to the long-term contact between the active material and the organic acid, the active material is easy to degrade, so it is necessary to wrap an isolation layer between the organic acid core and the active material, which makes the operation process more complicated and difficult to control. If the process is not properly operated, it is easy to The rupture of the isolation layer or the thickness of the isolation layer coating is not enough, so that the organic acid and the active substance come into contact due to diffusion during storage, resulting in the degradation of the active substance; and this prescription is mainly for patients with too little gastric acid secretion or gastric pH is too high, However, there are also many patients with excessive gastric acid secretion or low pH of gastric juice at the same time, such as patients with gastric diseases such as peptic ulcer and gastroesophageal reflux disease. Eating acidic substances can easily stimulate the stomach wall of these patients. Trigger gastric acid secretion, causing stomach discomfort and recurrence of the patient's condition

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1: Dabigatran etexilate dispersible tablet

[0037] Specifications: 1000 pieces

[0038]

[0039]

[0040] Coating Solution Prescription

[0041] Component Dosage

[0042] Opadry Coating Solution (03K19229) 100 parts

[0043] Purified water 1000ml

[0044] Preparation:

[0045] 1. Accurately weigh all the raw materials and auxiliary materials according to the prescription amount, and pass through a 100-mesh sieve. The disintegrant is divided into internally added and externally added parts, and the ratio of internally added and externally added parts is 4:1 (weight ratio); The extra parts are weighed and marked separately;

[0046] 2. Put the dabigatran etexilate mesylate raw material and all the internally added auxiliary materials in the mixer evenly; add the binder, continue mixing to make a suitable soft material, and granulate with a 30-mesh sieve;

[0047] 3. After the granules are dried at 40°C to 45°C, the water content is determi...

Embodiment 2

[0050] Embodiment 2 Dabigatran etexilate dispersible tablet

[0051] 1. Accurately weigh all the raw materials and auxiliary materials according to the prescription quantity, and pass through a 100-mesh sieve. The disintegrant is divided into internally added and externally added parts. The ratio of internally added and externally added parts is 3:2, and the weight ratio; internally added and externally added Parts are weighed and marked separately;

[0052] 2. Put the dabigatran etexilate mesylate raw material and all the internally added auxiliary materials in the mixer evenly; add the binder, continue mixing to make a suitable soft material, and granulate with a 30-mesh sieve;

[0053] 3. After the granules are dried at 40°C to 45°C, the water content is determined to be qualified, and the granules are sieved with a 30-mesh sieve.

[0054] 4. Add all the excipients according to the prescription amount, mix well, measure the particle content, calculate the tablet weight, ...

Embodiment 3

[0056] Embodiment 3 Dabigatran etexilate mesylate dispersible granule capsule

[0057] Specifications: 1000 pieces

[0058] Prescription:

[0059]

[0060] 1. Accurately weigh all raw materials and auxiliary materials according to the prescription amount, and pass through a 100-mesh sieve.

[0061] 2. Put the dabigatran etexilate mesylate raw material and all the internally added auxiliary materials in the mixer evenly; add the binder and continue mixing to make a suitable

[0062] 3. Soft material, granulated with 60 mesh sieve;

[0063] 4. After the granules are dried at 40°C to 45°C, the water content is determined to be qualified, and the granules are sieved with a 60-mesh sieve.

[0064] 5. Calculate the drug content of the obtained granules, weigh them accurately, and fill them in hollow capsules to obtain. The active substance content of each dabigatran etexilate sulfonate dispersible granule capsule is 150mg.

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Abstract

The invention relates to a dispersion preparation containing dabigatran etexilate. The dispersion preparation mainly comprises a dispersible tablet containing an active substance dabigatran etexilate, and a dispersed particle capsule. The preparation has the characteristics that the preparation can be disintegrated into fine particles in water within three minutes and a uniform suspension is formed. The particles can be evenly distributed and can pass through a 2# sieve (24 meshes). The dissolution rate and the absorption rate of the medicines can be significantly increased after the medicines with poor water solubility are prepared into the dispersion preparation, and the bioavailability is also improved. Meanwhile, the dispersion preparation has the advantages of being convenient to swallow, simple in production technology, high in reproducibility, high in medicine loading rate, easy to divide the dose and the like, and does not change the pH of gastric juice of a sufferer.

Description

technical field [0001] The invention relates to a dispersion preparation containing a salt or hydrate of dabigatran etexilate (active substance) and a preparation method and application thereof, belonging to the technical field of medicine. Background technique [0002] The chemical structure of the active substance dabigatran etexilate is 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H- Benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-ethyl propionate, the active substance is known from WO98 / 37075 and its chemical formula is shown in the following scheme I: [0003] [0004] Formula I [0005] The solubility of the active substance in water is lower than 5ug / ml, and the solubility of the active substance is greatly affected by pH, the solubility is higher under acidic conditions, and the solubility is significantly reduced when the pH>4. This compound is a non-peptidic direct thrombin inhibitor prodrug and has not shown any pharmacologic...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K9/48A61K31/4439A61K47/36A61P7/02
Inventor 郑春丽贾蕙丁亚飞刘建平朱家壁
Owner CHINA PHARM UNIV
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