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Apixaban tablet and preparation method thereof

A technology for apixaban tablets and tablet cores, applied in the field of medicine, can solve the problems of high impurity content and slow dissolution rate, and achieve the effects of simple technological process, low impurity content, and improved dissolution rate

Active Publication Date: 2015-04-08
HENAN RUNHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Chinese patent CN104095823 discloses a preparation method of apixaban tablet, which discloses that the tablet core of apixaban tablet is composed of apixaban, lactose, microcrystalline cellulose, cross-linked carboxymethyl cellulose Sodium, sodium lauryl sulfonate, magnesium stearate, the preparation method adopts firstly mixing and pulverizing apixaban and lactose, then adding other excipients and mixing, and then directly compressing the tablet, the prepared apixaban tablet dissolves for 15min The average dissolution rate can reach more than 80%, and the average dissolution rate can reach more than 90% after 30 minutes of dissolution, the dissolution speed is slow, and the impurity content is large

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

[0051] The apixaban tablet in this example includes a tablet core and a coating. The tablet core consists of the following components in percentage by weight: 2.6% of apixaban, 92.3% of lactose-cellulose complex, croscarmellose Sodium cellulose 3.1%, sodium lauryl sulfate 1.0%, magnesium stearate 1.0%;

[0052] The coating is made of the following components in mass percentage: hypromellose E56.01%, red iron oxide 0.1%, titanium dioxide 3.99%, and water 89.9%.

[0053] In this example, 1000 apixaban tablets were prepared, each apixaban tablet contained 5 mg of apixaban, and the coating weight was 2.6% to 5.4% of the tablet core weight.

[0054] The preparation method of the Apixaban tablet in this embodiment is, and the specific operation steps are:

[0055] 1) Micronizing 5.0 g of apixaban, controlling the particle size to be d90<10.0 μm, d50<4.0 μm, and d10<3.0 μm, to obtain apixaban micropowder;

[0056] 2) Premix the apixaban micropowder prepared in step 1) with 180.0 g ...

Embodiment 2

[0061] The apixaban tablet in this example includes a tablet core and a coating. The tablet core consists of the following components in percentage by weight: 2.6% of apixaban, 92.3% of lactose-cellulose complex, croscarmellose Sodium cellulose 3.1%, sodium lauryl sulfate 1.0%, magnesium stearate 1.0%;

[0062] The coating is made of the following components in mass percentage: hypromellose E56.01%, red iron oxide 0.1%, titanium dioxide 3.99%, and water 89.9%.

[0063] In this example, 1000 apixaban tablets were prepared, each containing 2.5 mg of apixaban, and the weight of the coating was 2.6% to 5.4% of the weight of the tablet core.

[0064] The preparation method of the Apixaban tablet in this embodiment is, and the specific operation steps are:

[0065] 1) Micronizing 2.5 g of apixaban, controlling the particle size to be d90<10.0 μm, d50<4.0 μm, and d10<3.0 μm, to obtain apixaban micropowder;

[0066] 2) Premix the apixaban micropowder prepared in step 1) with 90.0 g ...

Embodiment 3

[0071] The apixaban tablet in this example includes a tablet core and a coating, and the tablet core is composed of the following components in percentage by weight: 2.6% of apixaban, 92.1% of lactose-cellulose complex, croscarmellose Sodium cellulose 3.1%, sodium lauryl sulfate 1.1%, magnesium stearate 1.1%;

[0072] The coating is made of the following components in mass percentage: hypromellose E56.01%, red iron oxide 0.1%, titanium dioxide 3.99%, and water 89.9%.

[0073] In this example, 1000 apixaban tablets were prepared, each containing 2.5 mg of apixaban, and the weight of the coating was 2.6% to 5.4% of the weight of the tablet core.

[0074] The preparation method of the Apixaban tablet in this embodiment is, and the specific operation steps are:

[0075] 1) Micronize 2.5g of apixaban to control the particle size to d 90 50 10 <3.0μm, get apixaban micropowder;

[0076] 2) Premix the apixaban micropowder prepared in step 1) with 87.5 g of croscarmellose sodium, 3....

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Abstract

The invention discloses an apixaban tablet and a preparation method thereof, and belongs to the technical field of medicines. The apixaban tablet consists of a tablet core and a coating, wherein the tablet core is composed of apixaban, a fiber-lactose compound, crosslinked carboxy methyl cellulose, lauryl sodium sulfate and magnesium stearate; various components in the tablet core are controlled within limited dosage ranges and a mutual synergistic effect is achieved, so that the dosage of the cross-linked sodium carboxymethyl cellulose as a disintegrating agent is reduced and the dissolution rate of the apixaban tablet is improved; therefore, the average dissolution rate within 10min is more than 90%, the dissolution rate is slightly affected by illumination, temperature and humidity, the performance is stable, and the apixaban tablet is low in contents of impurities. According to the preparation method of the apixaban tablet disclosed by the invention, the tablet core is prepared by a way of directly tabletting a powdery mixture, so that a granulation process is avoided, operation is simple and convenient, and the technological process is simple; and the apixaban, as a crude drug, is subjected to micronization treatment before the mixed powder is prepared, so that the dissolution rate of the apixaban tablet is accelerated.

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, a new generation of oral antithrombotics, is a factor Xa inhibitor that can be used directly orally. It has been approved by European drug regulatory agencies and FDA for the prevention of adult patients undergoing elective hip or knee replacement The patient experienced a venous thromboembolic event. [0003] The chemical name of Apixaban is 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4, 5,6,7-Tetrahydro-1H-pyrido[3,4-c]pyridine-3-carboxamide, molecular formula C 25 h 25 N 5 o 4 , whose structural formula is: [0004] [0005] Apixaban is a white to light yellow crystalline powder with a solubility of 0.028mg / ml in water at 24°C and an average solubility of 0.040mg / ml in pH 1.2-pH6.8 aqueous solution at 37°C. Pixaban is a non-ionic compound, and its...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/4545A61K47/38A61P7/02
Inventor 高志亮
Owner HENAN RUNHONG PHARMA
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