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Imatinib mesylate tablet

A technology of imatinib mesylate tablets and imatinib mesylate, which is applied in the direction of pill delivery, medical preparations of non-active ingredients, organic active ingredients, etc., can solve the problems of strong viscosity, poor fluidity, and Poor pressure and other problems to achieve the effect of avoiding poor fluidity

Active Publication Date: 2012-01-04
SHANGHAI ACEBRIGHT PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The α crystal form of imatinib mesylate is currently considered unsuitable as a raw material for the preparation of pharmaceutical preparations due to its flocculent appearance, light weight, poor fluidity, poor compressibility, strong viscosity, and static electricity.
How to effectively avoid defects such as poor fluidity, poor compressibility, strong viscosity, and static electricity in the α crystal form of imatinib mesylate, and prepare stable and reliable formazan from the α crystal form of imatinib mesylate Imatinib sulfonate tablet is one of problems to be solved urgently in this area

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] formula:

[0020]

[0021] First, mix the formula amount of imatinib mesylate and magnesium carbonate in α crystal form and magnesium carbonate evenly, then add the formula amount of cross-linked polyvinylpyrrolidone to mix evenly, then add 70ml of ethanol to granulate, dry and add stearin Magnesium acid mixed, compressed into 1000 tablets.

[0022] According to the determination method of the angle of repose of the United States Pharmacopoeia USP32, the angle of repose of the particles measured is 35°.

[0023] The hardness, friability, disintegration time and dissolution rate of the prepared tablets were measured by a four-purpose tester for tablets. The measurement results are as follows: hardness 10KG; friability 0.4%; disintegration time 2 min;

[0024] Table 1

[0025] time (minutes)

Embodiment 2

[0027] formula:

[0028]

[0029] First, mix the formula amount of imatinib mesylate in α crystal form and magnesium carbonate evenly, then add the formula amount of cross-linked polyvinylpyrrolidone to mix evenly, then add 50ml of water to granulate, dry and add stearin Magnesium acid mixed, compressed into 1000 tablets.

[0030] According to the determination method of the angle of repose of the United States Pharmacopoeia USP32, the angle of repose of the particles measured is 33°.

[0031] The hardness, friability, disintegration time and dissolution rate of the prepared tablets were measured by a four-purpose tester for tablets. The measurement results are as follows: hardness 12KG; friability 0.5%; disintegration time 2.5 min;

[0032] Table 2

[0033] time (minutes)

Embodiment 3

[0035] formula:

[0036]

[0037] First, mix the formula amount of imatinib mesylate and magnesium carbonate in α crystal form evenly, then add the formula amount of cross-linked polyvinylpyrrolidone to make the mix evenly, then add 50ml of isopropanol to granulate, dry and add Magnesium stearate is blended and compressed into 1000 tablets.

[0038] According to the determination method of the angle of repose of USP32 of the United States Pharmacopoeia, the angle of repose of the particles measured is 40°.

[0039] The hardness, friability, disintegration time and dissolution rate of the prepared tablets were measured by a four-purpose tester for tablets. The measurement results are as follows: hardness 8KG; friability 0.8%; disintegration time 1.5 min;

[0040] table 3

[0041] time (minutes)

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Abstract

The invention discloses an imatinib mesylate tablet. The imatinib mesylate tablet comprises the following components in percentage by weight: 40-60% of alpha-crystal imatinib mesylate, 5-20% of antisticking agent, 20-50% of disintegrating agent and 0.2-1% of lubricating agent, wherein the sum of the weight percent of each component is 100%. According to the invention, through adding the antisticking agent, the defects of poor mobility, poor compressibility, poor stickness, static electricity and the like of alpha-crystal imatinib mesylate are avoided effectively; and the imatinib mesylate tablet prepared by alpha-crystal imatinib mesylate has consistent hardness, disintegration, dissolution and other quality standards with original tablet prepared by beta-crystal imatinib mesylate, and the detect that only beta-crystal imatinib mesylate is required as the raw material for preparing the imatinib mesylate tablet in the existing industry is solved.

Description

technical field [0001] The present invention relates to a kind of imatinib mesylate tablet, specifically, it relates to a kind of imatinib mesylate tablet prepared by using α crystal form imatinib mesylate as raw material, which belongs to medicine Formulation technology field. Background technique [0002] Imatinib mesylate, developed by Novartis, Switzerland, the chemical name is 4-(4-methyl-1-piperazine)methyl-N-4-methyl-3-4-(3-pyridine)- 2-Pyrimidineaminophenyl-aniline methanesulfonate, molecular formula C 29 h 31 N 7 O·CH 4 SO 3 , the molecular weight is 589.7, and the chemical structural formula is: It can be used for the treatment of chronic myelogenous leukemia (CML) in the blast phase, accelerated phase or chronic phase after failure of α-interferon therapy; patients with malignant gastrointestinal stromal tumor (GIST) that cannot be surgically removed or has metastasized. [0003] International patent application WO 99 / 03854 discloses that there are two cry...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/506A61K47/38A61K47/36A61K47/32A61P35/02A61P35/00
CPCA61K9/2059A61K9/20A61K47/36A61K9/2027A61K9/2009A61K47/32A61K47/38A61K9/2054A61K31/506A61P35/00A61P35/02
Inventor 安晓霞张静李小强马素伟
Owner SHANGHAI ACEBRIGHT PHARMA CO LTD
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