Method for preparing apixaban tablets

A technology for apixaban tablets and lubricants, which is applied in the field of preparation of apixaban tablets, can solve the problems of low in vitro dissolution rate, low bioavailability, and slow dissolution rate, and achieve high bioavailability and preparation The effect of simple method and low packaging cost

Inactive Publication Date: 2015-04-08
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 ...

Method used

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  • Method for preparing apixaban tablets
  • Method for preparing apixaban tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Components of apixaban tablets

[0029] Component

Dose 1 (mg)

Dose 2 (mg)

Dose 3 (mg)

Apixaban

10

20

30

Microcrystalline fiber

38

76

114

Anhydrous lactose

70

140

210

Crosslinked Sodium Cellulose

2

4

6

Sodium dodecyl sulfate

2

4

6

Magnesium stearate

0.2

0.4

0.6

[0030] Preparation:

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

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

Embodiment 2

[0034] Apixaban tablet components

[0035] Component

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:

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

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

Embodiment 3

[0040] Components of apixaban tablets

[0041]

[0042] Preparation:

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

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

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Abstract

The invention relates to a method for preparing apixaban tablets. The method comprises the following steps: (1) uniformly mixing apixaban, an excipient, a disintegrating agent, a surfactant and a lubricating agent, performing wet granulation, screening the prepared soft material by using a 20-mesh sieve, granulating, drying and finishing the obtained particles, and collecting the dried particles with the particle size being between 20 meshes and 80 meshes; and (2) mixing the prepared particles with the lubricating agent for 30 minutes and tabletting, wherein the hardness of the tablets is 50-60N. In order to improve the dissolubility, a method for adding the surfactant into the prescription is adopted. According to the method, the dissolubility of the apixaban can be improved, and the problem is well solved, so that the bioavailability of the medicine is improved, and an excellent treatment effect is achieved.

Description

Technical field [0001] The invention belongs to the technical field of western medicine preparations, and particularly relates to a preparation method of apixaban tablets. Background technique [0002] Agaoxaban is a new type of oral direct factor Xa inhibitor with the chemical formula of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl) ) Phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-methideamine. The molecular formula is C25H25N5O4 and the molecular weight is 459.50. The structural formula is as follows: [0003] [0004] Atrial fibrillation (AF) is the most common type of arrhythmia clinically, and it is an important independent risk factor for stroke. AF patients are at risk of cerebral embolism or transient ischemic attack (TIA) in non-AF patients 4-5 times. In addition, patients with AF usually have poorer stroke outcomes and higher mortality and disability rates. The fatality rate of AF patients within 1 year after stroke is as high as 50%. Therefore, it i...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4545A61K47/34A61K47/20A61P9/06
Inventor 权超陈林
Owner TIANJIN YIYAO SCI & TECH
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