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Apixaban tablet and preparation method thereof

A technology for apixaban tablets and excipients, applied in the field of apixaban tablets and its preparation, can solve the problems of low in vitro dissolution rate, low bioavailability, slow dissolution rate, etc., and achieve simple preparation process, The effect of high bioavailability and low packaging cost

Inactive Publication Date: 2015-04-22
TIANJIN YIYAO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Apixaban itself is insoluble in water, has the disadvantages of slow dissolution rate, low in vitro dissolution rate, and low bioavailability, which have a certain impact on the absorption of human body

Method used

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  • Apixaban tablet and preparation method thereof
  • Apixaban tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Components of Apixaban Tablets

[0029] components

Dose 1 (mg)

Dose 2 (mg)

Dose 3 (mg)

Apixaban

10

20

30

microcrystalline fiber

38

76

114

anhydrous lactose

70

140

210

Crosslinked Cellulose Sodium

2

4

6

Sodium dodecyl sulfate

2

4

6

Magnesium stearate

0.2

0.4

0.6

[0030] Preparation Process:

[0031] (1) Weigh the raw and auxiliary materials of the above prescription amount, except for magnesium stearate, mix all the raw and auxiliary materials and carry out wet granulation. The soft material obtained is granulated with a 20-mesh sieve, and the obtained granules are dried and granulated. Granules, and finally collect dry particles between 20 mesh and 80 mesh.

[0032] (2) After mixing the prepared granules with magnesium stearate for 30 minutes, press into tablets, and the hardness of the tablets is 50-60N.

Embodiment 2

[0034] Apixaban Tablet Ingredients

[0035] components

Dose 1 (mg)

Dose 2 (mg)

Dose 3 (mg)

Apixaban

10

20

40

powdered sugar

60

120

250

microcrystalline fiber

22

40

88

Crospovidone

3

6

16

Sodium dodecyl sulfonate

2

4

6

Magnesium stearate

0.2

0.4

0.6

[0036] Preparation Process:

[0037] (1) Weigh the raw and auxiliary materials of the above prescription amount, except for magnesium stearate, mix all the raw and auxiliary materials and carry out wet granulation. The soft material obtained is granulated with a 20-mesh sieve, and the obtained granules are dried and granulated. Granules, and finally collect dry particles between 20 mesh and 80 mesh.

[0038] (2) After mixing the prepared granules with magnesium stearate for 30 minutes, press into tablets, and the hardness of the tablets is 50-60N.

Embodiment 3

[0040] Components of Apixaban Tablets

[0041]

[0042] Preparation Process:

[0043] (1) Weigh the raw and auxiliary materials of the above prescription amount, except for magnesium stearate, mix all the raw and auxiliary materials and carry out wet granulation. The soft material obtained is granulated with a 20-mesh sieve, and the obtained granules are dried and granulated. Granules, and finally collect dry particles between 20 mesh and 80 mesh.

[0044] (2) After mixing the prepared granules with magnesium stearate for 30 minutes, press into tablets, and the hardness of the tablets is 50-60N.

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Abstract

The invention discloses an apixaban tablet comprising the raw materials including apixaban, an excipient, a disintegrating agent, a surfactant and a lubricant in a weight ratio of (5-20):(0.5-2.5):(0.1-0.3):(0.1-2.0). In order to improve the dissolution degree of the apixaban tablet disclosed by the invention, a method for adding the surfactant into the formula is adopted, and the method can increase the dissolution degree of apixaban, so that the problem is well solved, the bioavailability of the medicament is improved, and a very good curative effect is achieved.

Description

technical field [0001] The invention belongs to the technical field of western medicine preparations, in particular to an apixaban tablet and a preparation method thereof. Background technique [0002] Aguaxaban 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. The molecular formula is C25H25N5O4 and the molecular weight is 459.50. The structural formula is as follows: [0003] [0004] Atrial fibrillation (atrial fibrillation, AF) is the most common type of arrhythmia clinically, and it is an important independent risk factor for stroke. The risk of cerebral embolism or transient ischemic attack (TIA) in AF patients is higher than that in non-AF patients. 4-5 times. In addition, stroke outcomes in patients with AF are generally poorer, with higher rates of mortality and disability. The mortality rate of AF patients within 1 ye...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4545A61K47/34A61K47/20A61P7/02A61P9/10
Inventor 权超陈林
Owner TIANJIN YIYAO SCI & TECH
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