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A kind of Afatinib maleate tablet and preparation method thereof

A technology of afatinib and maleic acid, which is applied in the field of medicine, can solve the problems of low hardness, long production cycle, and high friability, and achieve the effects of improving stability, fluidity, and dissolution

Active Publication Date: 2020-07-14
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, freeze-dried tablets have low hardness and high friability, and the tablets are easily broken during transportation.
At the same time, the freeze-drying process is complicated, the production cycle is long, the efficiency is low, the cost is high, and it is difficult to produce on a large scale
And, afatinib maleate is poor in stability in aqueous solution, is difficult for adopting this technique to prepare
[0011] In the prior art, afatinib maleate tablets with good stability, rapid dissolution and simple preparation process have not been provided yet.

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] prescription:

[0037]

[0038] Preparation Process:

[0039] ⅰ Dissolve afatinib maleate and menthol in an ethanol solution, cool the solution to -5°C for crystallization under continuous stirring, and obtain complex crystals. Weigh the complex crystals and mix them with mannitol. Add The magnesium stearate is mixed evenly to obtain afatinib maleate tableting mixed powder;

[0040] ⅱThe mixed powder prepared by ⅰ is punched with Ф9mm shallow arc;

[0041] ⅲPut the prepared tablet into an oven for heat treatment at 40°C for 12h;

[0042] iv. The heat-treated tablet of iii is coated with a stomach-dissolving film, and then packaged.

Embodiment 2

[0044] prescription:

[0045]

[0046]

[0047] Preparation Process:

[0048] ⅰ Dissolve afatinib maleate and menthol in ethanol solution, cool the solution to -5°C for crystallization under continuous stirring, and obtain compound crystals. Weigh the compound crystals and mix them with lactose uniformly. Magnesium fatty acid is mixed evenly to obtain afatinib maleate tableting mixed powder;

[0049] ⅱThe mixed powder prepared by ⅰ is punched with Ф9mm shallow arc;

[0050] ⅲPut the prepared tablet into an oven and heat treatment at 50°C for 10h;

[0051] iv. The heat-treated tablet of iii is coated with a stomach-dissolving film, and then packaged.

Embodiment 3

[0053] prescription:

[0054]

[0055] Preparation Process:

[0056]ⅰ Dissolve afatinib maleate and menthol in an ethanol solution, cool the solution to -5°C for crystallization under continuous stirring to obtain a complex crystal, weigh the complex crystal and mix it with sorbitol evenly, add Calcium stearate is mixed evenly to obtain afatinib maleate tableting mixed powder;

[0057] ⅱThe mixed powder prepared by ⅰ is punched with Ф9mm shallow arc;

[0058] ⅲPut the prepared tablet into an oven for heat treatment at 60°C for 8h;

[0059] iv. The heat-treated tablet of iii is coated with a stomach-dissolving film, and then packaged.

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PUM

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Abstract

The present invention provides an afatinib dimaleate tablet and a preparation method thereof, wherein the preparation does not contain a disintegrating agent. According to the present invention, afatinib dimaleate and a menthol ethanol solution are subjected to cooling crystallization to obtain a complex crystal, the complex crystal, a water-soluble filler and a lubricant are subjected to mixing tableting, most of the menthol is removed through heat treatment, and coating with a gastric soluble film is performed to prepare the afatinib dimaleate tablet; and the prepared afatinib dimaleate tablet has advantages of rapid dissolution and good stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to afatinib maleate tablet and a preparation method thereof. Background technique [0002] The original manufacturer of afatinib maleate is Boehringer Ingelheim, Germany, which was approved by FDA and EMA in July 2013. The dosage form is film-coated tablets, with specifications of 20mg, 30mg and 40mg. Afatinib maleate is approved in the EU under the trade name GIOTRIF for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) mutations. Approved in the U.S. under the trade name GILOTRIF as first-line therapy for metastases with epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations detected by an FDA-approved assay patients with non-small cell lung cancer (NSCLC). [0003] Afatinib maleate is white to yellow-brown powder, slightly hygroscopic, and has good w...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/28A61K31/517A61K47/10A61P35/00
CPCA61K9/2013A61K9/2018A61K9/28A61K31/517
Inventor 张贵民陈小伟耿兴锴闫勋栋
Owner SHANDONG NEWTIME PHARMA
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