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Afatinib dimaleate tablet and preparation method thereof

A technology of tinib tablet and maleic acid, which is applied in the field of afatinib maleate tablet and its preparation, can solve the problems of poor powder fluidity, lobes, large differences in tablet weight, etc., and achieve adjustment of bulk density, improvement of Fluidity, effect of improving solubility performance

Inactive Publication Date: 2016-11-09
NANJING CHENGONG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the powder direct compression method faces many challenges: 1) The type and dosage of active ingredients and excipients are very picky; 2) The fluidity of the powder is poor; 3) The tablet weight varies greatly; 4) It is easy to cause splits

Method used

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  • Afatinib dimaleate tablet and preparation method thereof
  • Afatinib dimaleate tablet and preparation method thereof
  • Afatinib dimaleate tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The afatinib maleate tablet in the present embodiment is made up of a tablet core and a film coating wrapped outside the tablet core, and the tablet core is made of raw materials of the following quality (1000 tablets, afatinib 40mg / tablet) : Afatinib maleate (calculated as afatinib) 59.12g, lactose monohydrate 230.0g, microcrystalline cellulose 42.0g PH301, crospovidone 18.0g, silicon dioxide 2.0g, stearic acid Magnesium 6.0g; film coating adopts the following quality raw materials (1000 tablets): 10.0g, water 152.0g.

[0021] Preparation method: Accurately take the raw and auxiliary materials according to the parts by mass, first mix afatinib maleate, lactose monohydrate, microcrystalline cellulose PH301, crospovidone, and silicon dioxide for 20 minutes, then add stearic acid Magnesium, mixed for 10 minutes, prepared granules by roller compaction, adding magnesium stearate to the prepared granules, mixed for 20 minutes, compressed into tablets to obtain tablet cores. ...

Embodiment 2

[0023] The afatinib maleate tablet in the present embodiment is made up of a tablet core and a film coating wrapped outside the tablet core, and the tablet core is made of raw materials of the following quality (1000 tablets, afatinib 40mg / tablet) : Afatinib maleate (calculated as afatinib) 59.12g, lactose monohydrate 235.0g, microcrystalline cellulose PH103 45.0g, crospovidone 20.0g, silicon dioxide 2.2g, stearic acid Magnesium 7.0g; film coating adopts the following quality raw materials (1000 tablets): 12.0g, water 156.0g.

[0024] Preparation method: Accurately take the raw and auxiliary materials according to the parts by mass, first mix afatinib maleate, lactose monohydrate, microcrystalline cellulose PH301, crospovidone, and silicon dioxide for 20 minutes, then add stearic acid Magnesium, mixed for 10 minutes, prepared granules by roller compaction, adding magnesium stearate to the prepared granules, mixed for 20 minutes, compressed into tablets to obtain tablet cores. ...

Embodiment 3

[0026] The afatinib maleate tablet in the present embodiment is made up of tablet core and the film coating that is wrapped in outside the tablet core, and tablet core is made of the raw material of following quality (1000 tablets, afatinib 30mg / tablet) : Afatinib maleate (calculated as afatinib) 44.34g, lactose monohydrate 172.5g, microcrystalline cellulose PH-F20 31.5g, crospovidone 13.5g, silicon dioxide 1.5g, hard Magnesium fatty acid 4.5g; film coating adopts the following quality raw materials (1000 tablets): 7.5g, water 114.0g.

[0027]Preparation method: Accurately take the raw and auxiliary materials according to the parts by mass, first mix afatinib maleate, lactose monohydrate, microcrystalline cellulose PH301, crospovidone, and silicon dioxide for 20 minutes, then add stearic acid Magnesium, mixed for 10 minutes, prepared granules by roller compaction, adding magnesium stearate to the prepared granules, mixed for 20 minutes, compressed into tablets to obtain table...

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Abstract

The invention provides an afatinib dimaleate tablet and a preparation method thereof. The afatinib dimaleate tablet is composed of a table core and a film coating wrapping the exterior of the table core and prepared by taking lactose monohydrate and microcrystalline cellulose PH301 as filling agents, taking crospovidone as a disintegrating agent, taking silicon dioxide as a flow aid and taking magnesium stearate as a lubricating agent. The preparation method has the advantages that the tablet is prepared by adopting a dry granulation technique, the fluidity can be improved, separation of all the components can be prevented to avoid the condition that the tablet components are not uniform, the bulk density is regulated, and the dissolving property and uniform pressure transmission in tablet production are improved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a maleic acid afatinib tablet and a preparation method thereof. Background technique [0002] Afatinib Dimaleate (CAS: 850140-73-7), chemical name: 4-dimethylamino-but-2(E)-enoic acid [4-(3-chloro-4-fluoro Anilino)-7-(tetrahydrofuran-3(S)-oxygen)-quinazolin-6-yl]amide two-2(Z)-butenediol, molecular formula is: C24H25ClFN5O3 2C4H4O4 Molecular weight is salt 718.1( dimaleinate) base 486.0, afatinib maleate is off-white to yellowish-white solid substance; there is an ionizable group, so it can be observed that it has a lipophilic character with strong pH dependence; it has hygroscopicity and can reach a relative humidity of More than 70% of the environment can absorb water; in the water-soluble medium with a pH value as high as 7, it shows high solubility, and when the pH value of the medium is higher than 8, its solubility decreases significantly; in anhydrous ...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K31/517A61K47/26A61K47/38A61K47/04A61K47/12A61P35/00
CPCA61K9/286A61K9/2009A61K9/2018A61K9/2054A61K9/2095A61K31/517
Inventor 何金凤薛娟白中稳刘斐孙松
Owner NANJING CHENGONG PHARM CO LTD
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