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Imatinib mesylate composition and preparation method thereof

A technology of imatinib mesylate and imatinib mesylate, which is applied in the field of imatinib mesylate tablet and its preparation, can solve the problem of incomplete dissolution of tablets, prolonging the stimulation journey, and irritation of the digestive tract and other problems, to achieve the effect of shortening the granulation time, improving safety and high dissolution rate

Active Publication Date: 2012-02-15
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And according to The dissolution of the tablet prepared by the disclosed method is incomplete or slow, and under the dissolution condition of 0.1M HCL 1000ml / 50rpm (paddle method), the dissolution rate in 10min is less than 60%.
[0013] Oral medicine is absorbed in a dissolved state after entering the body, and imatinib mesylate itself is easily soluble. The crystal form of imatinib mesylate in the present invention is a stable β crystal form, and it is not necessary to adopt complicated technological means to prepare into solid solution, solid dispersion or clathrate; imatinib mesylate has a bitter taste and is irritating to the digestive tract. It is not necessary and not suitable for making chewable tablets or orally disintegrating tablets, because these two preparations will prolong the irritation journey; the production of effervescent tablets requires special environmental requirements, and taking effervescent tablets will also prolong the stimulation journey
[0014] It is hoped that imatinib mesylate can quickly reach the blood concentration and take effect after taking it, but the prior art fails to provide an imatinib mesylate drug with simple composition and preparation process that can realize rapid drug release combination

Method used

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  • Imatinib mesylate composition and preparation method thereof
  • Imatinib mesylate composition and preparation method thereof
  • Imatinib mesylate composition and preparation method thereof

Examples

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Effect test

Embodiment 1～3

[0036]

[0037] Preparation Process:

[0038] i) passing imatinib mesylate, microcrystalline cellulose and crospovidone through a 60-mesh sieve for subsequent use;

[0039] ii) Weighing imatinib mesylate, microcrystalline cellulose and the crospovidone added in part are mixed uniformly;

[0040] iii) take by weighing the silicon dioxide and magnesium stearate of adding part, mix homogeneously;

[0041] iv) dry granulator granulation, pressure 5MPa;

[0042] v) According to the proportion of the prescription, add the excipients and mix them evenly;

[0043] vi) Compressed into tablets with a hardness of 6-8kg / cm 2 .

Embodiment 4

[0045] Prescription is the same as embodiment 1

[0046] Preparation Process:

[0047] i) imatinib mesylate is passed through a 200 mesh sieve, and microcrystalline cellulose and crospovidone are passed through a 60 mesh sieve for subsequent use;

[0048] ii) Weighing imatinib mesylate, microcrystalline cellulose and the crospovidone added in part are mixed uniformly;

[0049] iii) take by weighing the silicon dioxide and magnesium stearate of adding part, mix homogeneously;

[0050] iv) dry granulator granulation, pressure 5MPa;

[0051] v) According to the proportion of the prescription, add the excipients and mix them evenly;

[0052] vi) Compressed into tablets with a hardness of 6-8kg / cm 2 .

Embodiment 5

[0054] The tablet prepared in Example 1 was coated with Opadry.

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Abstract

The invention provides an imatinib mesylate composition and a preparation method thereof. The imatinib mesylate composition is prepared from imatinib mesylate used as an active ingredient through a dry granulation process, and the dissolution rate of imatinib mesylate is effectively improved.

Description

technical field [0001] The invention relates to a composition of imatinib mesylate, in particular to an imatinib mesylate tablet capable of rapidly releasing medicine and a preparation method thereof. Background technique [0002] Imatinib mesylate is a selective tyrosine kinase inhibitor developed by Swiss Novartis, which belongs to the anilinoquinazoline compounds. It was approved by FDA in May 2001 for the treatment of chronic myelogenous leukemia. In February 2002, FDA further approved imatinib mesylate for the treatment of gastrointestinal stromal tumors. [0003] Imatinib mesylate can inhibit Bcr-Abl tyrosine kinase at the cellular level in vivo and in vitro, and can selectively inhibit Bcr-Abl positive cell line cells, Ph chromosome-positive chronic myeloid leukemia and acute lymphoblastic leukemia Proliferation and induction of apoptosis in fresh cells from patients. In addition, imatinib mesylate can also inhibit platelet-derived growth factor (PDGF) receptor, ste...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/506A61K47/36A61P35/02
Inventor 张志宏金丽丽辛伟张素娟陈勇军杨丽霞
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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