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A kind of preparation method of Afatinib maleate tablet

A technology of maleic acid and alpha, which is applied in the field of preparation of maleic acid afatinib tablets to achieve the effects of improving stability, avoiding drying, and uniform content

Active Publication Date: 2018-02-23
GUANGDONG ANNOL PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no relevant report about the application of hot-melt granulation method to prepare afatinib maleate tablets

Method used

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  • A kind of preparation method of Afatinib maleate tablet
  • A kind of preparation method of Afatinib maleate tablet
  • A kind of preparation method of Afatinib maleate tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3 and comparative example 1-10

[0041] The preparation of embodiment 1-3 and comparative example 1-10 Afatinib maleate sheet

Embodiment 1-3

[0042] Example 1-3 The composition of Afatinib Maleate Tablets is shown in the table below:

[0043]

[0044]

Embodiment 1

[0049] Example 1 Preparation of Afatinib Maleate Tablets:

[0050] (1) In parts by weight, take respectively afatinib maleate 29.56g, mannitol 118g, microcrystalline cellulose PH10124g, polyethylene glycol PEG6000 30g, calcium sulfate 10g, crospovidone 3.6g, Magnesium stearate 0.5g, silicon dioxide 2g, stomach-soluble film coating premix ( 295B680002) 5.4g, spare;

[0051] (2) Mix afatinib maleate, mannitol, microcrystalline cellulose PH101, polyethylene glycol PEG6000 and calcium sulfate (2.5g) evenly, heat to 70°C, keep warm for 15 minutes after reaching the predetermined temperature, Cool at room temperature, add crospovidone, extra calcium sulfate (7.5g), magnesium stearate, and silicon dioxide after granulation, mix evenly, and compress into tablets;

[0052] (3) Use the gastric-soluble film coating premix ( 295B680002) was film-coated to obtain Afatinib maleate tablets.

[0053] Examples 2 and 3 The preparation of afatinib maleate tablets is shown in reference ...

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Abstract

The invention discloses a preparation method of afatinib dimaleate tablets. The preparation method comprises the following steps: 1) respectively weighing raw materials in parts by weight; 2) uniformly mixing afatinib dimaleate, a diluting agent, polyethylene glycol and internal calcium sulfate, heating to 60 to 70 DEG C, after the mixture reaches a predetermined temperature, keeping the temperature for 10 to 15min, cooling at room temperature, granulating, adding and uniformly mixing a disintegrating agent, external calcium sulfate, magnesium stearate and silicon dioxide, and tabletting; and 3) coating the tablets, thus obtaining the afatinib dimaleate tablet. The obtained tablets are stable in quality, uniform in content and good in in-vitro dissolution behavior.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a preparation method of afatinib maleate tablets. Background technique [0002] Afatinib maleate was developed by Boehringer-Ingelheim and was approved by the US Food and Drug Administration (FDA) on July 12, 2013, and then approved by the European Drug Administration on September 25, 2013. Approved by the EMA for listing, it was approved for listing by the Japan Pharmaceuticals and Medical Devices Agency (PMDA) on January 17, 2014. It is marketed by Boehringer Ingelheim. The product is [0003] The chemical name of afatinib maleate is: 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo -2-buten-1-yl]amino}-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline dimaleate, the structural formula is: [0004] [0005] Molecular formula: C 32 h 33 ClFN 5 o 11 , Molecular weight: 718.1, white to brown yellow powder, easily soluble in wa...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/36A61K31/517A61K47/10A61K47/38A61K47/02A61P35/00
CPCA61K9/2009A61K9/2018A61K9/2054A61K9/2095A61K9/2866A61K31/517
Inventor 龙世松曹祺
Owner GUANGDONG ANNOL PHARM CO LTD
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