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Apixaban tablet

A technology of apixaban tablet and water-soluble carrier, which is applied in the field of medicine, can solve the problems of drug absorption influence, low in vitro dissolution rate, low bioavailability, etc., and achieves convenience for large-scale production, good reproducibility, and increased drug absorption effect

Inactive Publication Date: 2013-02-06
NANJING ZENKOM PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Apixaban is insoluble in water, has the disadvantages of slow dissolution rate, low in vitro dissolution rate, and low bioavailability, which has a certain impact on drug absorption
In order to improve the dissolution rate of apixaban, the method of adding a large amount of surfactants to the prescription is generally adopted. Although this method can increase the dissolution rate of apixaban, a large amount of surfactants will bring a large amount of toxic and side effects to the human body.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] This example provides the prescription and preparation method for preparing 10,000 Apixaban tablets (specification: 2.5 mg / tablet) as follows

[0022] Preparation:

[0023] (1) Take polyethylene glycol 6000 of recipe quantity, heat to melt at 60 ℃;

[0024] (2) Add the apixaban of the prescribed amount into the melt obtained in step (1) under slow stirring conditions, stir vigorously after adding all of it, the slow stirring is 200~400r / min, and the vigorous stirring is 10000~20000r / min;

[0025] (3) rapidly cooling and solidifying the melt obtained in step (2) for 2 hours at -20°C;

[0026] (4) Grinding the cured product obtained in step (3) at 0°C and passing through an 80-mesh sieve; drying the crushed product at 20°C for 4 hours under reduced pressure to obtain apixaban solid dispersion;

[0027] (5) Mix the apixaban solid dispersion obtained in the step (4) with the prescribed amount of microcrystalline cellulose; crospovidone; and micropowdered silica gel eve...

Embodiment 2

[0029] This example provides the prescription and preparation method for preparing 10,000 Apixaban tablets (specification: 2.5 mg / tablet) as follows

[0030] Preparation:

[0031] (1) Take polyethylene glycol 6000 of recipe quantity, heat to melt at 60 ℃;

[0032] (2) Add the apixaban of the prescribed amount into the melt obtained in step (1) under slow stirring conditions, stir vigorously after adding all of it, the slow stirring is 200~400r / min, and the vigorous stirring is 10000~20000r / min;

[0033] (3) rapidly cooling and solidifying the melt obtained in step (2) for 2 hours at -20°C;

[0034] (4) Grinding the cured product obtained in step (3) at 0°C and passing through an 80-mesh sieve; drying the crushed product at 20°C for 4 hours under reduced pressure to obtain apixaban solid dispersion;

[0035] (5) Mix the apixaban solid dispersion obtained in the step (4) with the prescribed amount of microcrystalline cellulose; crospovidone; and micropowdered silica gel eve...

Embodiment 3

[0037] This example provides the prescription and preparation method for preparing 10,000 Apixaban tablets (specification: 2.5 mg / tablet) as follows

[0038] Preparation:

[0039] (1) Take polyethylene glycol 6000 of recipe quantity, heat to melt at 60 ℃;

[0040] (2) Add the apixaban of the prescribed amount into the melt obtained in step (1) under slow stirring conditions, stir vigorously after adding all of it, the slow stirring is 200~400r / min, and the vigorous stirring is 10000~20000r / min;

[0041] (3) rapidly cooling and solidifying the melt obtained in step (2) for 2 hours at -20°C;

[0042] (4) Grinding the cured product obtained in step (3) at 0°C and passing through an 80-mesh sieve; drying the crushed product at 20°C for 4 hours under reduced pressure to obtain apixaban solid dispersion;

[0043] (5) Mix the apixaban solid dispersion obtained in the step (4) with the prescribed amount of microcrystalline cellulose; crospovidone; and micropowdered silica gel eve...

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Abstract

The invention discloses an Apixaban tablet, which comprises the following components in parts: 1 part of Apixaban, 10-20 parts of water-soluble carrier material, 30-60 parts of filling agent, 5-10 parts of disintegrating agent and 5-10 parts of glidant. The Apixaban tablet provided by the invention improves the deficiencies in the prior art that the extracorporeal dissolution rate and the bioavailability is low. The preparation method of the Apixaban tablet disclosed by the invention is simple to operate, has good reproducibility, and is suitable for large-scale production. The Apixaban tablet is mainly used for the anti-thrombosis purpose.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an apixaban tablet and a preparation method thereof. Background technique [0002] Apixaban is a novel oral direct factor Xa inhibitor with the chemical formula 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl) )phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide. Molecular formula is C 25 h 25 N 5 o 4 , the molecular weight is 459.50. The structural formula is as follows: [0003] [0004] Cardiovascular and cerebrovascular diseases are characterized by their high incidence, high recurrence rate, high disability rate, and high mortality rate, which have seriously threatened people's health. At present, one out of every five adults in my country suffers from cardiovascular and cerebrovascular diseases, and one person dies from cardiovascular and cerebrovascular diseases every 10 seconds. The number of deaths due to cerebrovascular disease...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4545A61P7/02
Inventor 祁艳徐卓业
Owner NANJING ZENKOM PHARMA
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