Apixaban tablet and preparation method thereof

A technology of apixaban tablets and apixaban, which is applied in the field of medicine, can solve problems such as safety to be considered, achieve the effects of increasing stability and degradation of impurities, simple production process, and easy large-scale production

Inactive Publication Date: 2018-06-01
NANJING ZENKOM PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since diethylene glycol monoethyl ether is a flammable liquid and has certain toxicity, the safety needs to be considered

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] This example provides the prescription and preparation method for preparing 10,000 Apixaban tablets as follows

[0027]

[0028]

[0029] Preparation:

[0030] (1) Take by weighing the mannitol of recipe quantity, 170 ℃ are heated to melting;

[0031] (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;

[0032] (3) rapidly cooling and solidifying the melt obtained in step (2) for 2 hours at -20°C;

[0033] (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;

[0034] (5) Mix the apixaban solid dispersion obtained in the step (4) with the prescribed amount of microcrystalline cellulose; crospovidone; and micropowdered silica gel evenl...

Embodiment 2

[0036] This example provides the prescription and preparation method for preparing 10,000 Apixaban tablets as follows

[0037]

[0038] Preparation:

[0039] (1) Take by weighing the mannitol of recipe quantity, 170 ℃ are heated to melting;

[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 evenly and direct...

Embodiment 3

[0045] This example provides the prescription and preparation method for preparing 10,000 Apixaban tablets as follows

[0046]

[0047] Preparation:

[0048] (1) Take by weighing the mannitol of recipe quantity, 170 ℃ are heated to melting;

[0049] (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;

[0050] (3) rapidly cooling and solidifying the melt obtained in step (2) for 2 hours at -20°C;

[0051] (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;

[0052] (5) Mix the apixaban solid dispersion obtained in the step (4) with the prescribed amount of microcrystalline cellulose; crospovidone; and micropowdered silica gel evenly and directly...

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PUM

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Abstract

The invention discloses an apixaban tablet. The apixaban tablet is formed through tableting of apixaban solid dispersion and auxiliary ingredients, wherein the apixaban solid dispersion is formed by apixaban and mannitol at the weight ratio of 1 to (10-20); the auxiliary ingredients comprise microcrystalline cellulose, polyvinylpolypyrrolidone and superfine silica powder, and the weight ratio of apixaban to microcrystalline cellulose to polyvinylpolypyrrolidone to the superfine silica powder is 1 to (30-60) to (5-10) to (1-5). With the apixaban tablet provided by the invention, the defects that the in-vitro dissolution rate of apixaban is poor and the bioavailability is low are overcome. The invention further discloses a preparation method of the apixaban tablet. The method is easy to operate, the reproducibility is good, and large-batch production can be easily realized. The apixaban tablet is mainly used for resisting thrombus.

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 l-(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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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4545A61K47/26A61P7/02A61P9/10
CPCA61K9/2018A61K31/4545
Inventor 祁艳徐卓业
Owner NANJING ZENKOM PHARMA
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