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Medicinal preparation containing crystal form a imatinib mesylate

A technology for imatinib mesylate and pharmaceutical preparations, which is applied in the field of pharmaceutical preparations containing α-crystalline imatinib mesylate, and can solve the problems of unsuitable physical properties for preparations, large proportions of main ingredients, and changes in Properties of pharmaceutical preparations, etc.

Inactive Publication Date: 2012-07-11
TIANJIN TAIPU PHARMA SCI & TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the α crystal form of imatinib mesylate, its inherent physical properties are not suitable for formulation
And because the dosage of imatinib mesylate is very large, the proportion of the main drug in the pharmaceutical preparation is very large, it is difficult to use a large number of excipients to change the properties of the pharmaceutical preparation

Method used

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  • Medicinal preparation containing crystal form a imatinib mesylate
  • Medicinal preparation containing crystal form a imatinib mesylate
  • Medicinal preparation containing crystal form a imatinib mesylate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] 100mg Imatinib Mesylate Tablets

[0045] prescription:

[0046]

[0047] In the table *: 119.5 mg of imatinib mesylate, calculated as 100 mg of imatinib. In the table, 1 represents internal auxiliary materials, and 2 represents external auxiliary materials.

[0048] Preparation Process:

[0049] Pulverize imatinib mesylate in α crystal form, mix with the auxiliary materials added in and pass through a 60-mesh sieve; add absolute ethanol, mix in a high-speed shear mixer, use a 40-mesh sieve (0.425mm) to make granules, and use The oven dries the wet granules. Thoroughly mix dry granules with additional excipients. The blend was directly compressed (see Figure 2).

Embodiment 2

[0051] This embodiment uses isopropanol as a binder, and the purpose is to compare with Embodiment 1.

[0052] Prescription: with embodiment 1

[0053] Process: Grind the α-crystalline imatinib mesylate, mix it with the added PVPP, and pass through a 60-mesh sieve; add isopropanol, mix in a high-speed shear mixer, use a 40-mesh sieve to make granules, and use an oven to sieve Wet granules dry.

Embodiment 3

[0055] In this example, 98% ethanol is used as a binder, and the purpose is to compare with Example 1.

[0056] Prescription: with embodiment 1

[0057] Process: Pulverize imatinib mesylate in α crystal form, mix it with the added PVPP and pass through a 60-mesh sieve; add 98% ethanol, mix in a high-speed shear mixer, use a 40-mesh sieve to make granules, and use an oven to sieve Wet granules dry.

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Abstract

The invention discloses a medicinal preparation containing crystal form a imatinib mesylate. The medicinal preparation comprises crystal form a imatinib mesylate, a disintegrating agent, a diluent, a lubricating agent and a flow aid, wherein the using amount of the imatinib mesylate accounts for 50-80 percent of the total weight of the medicinal preparation; the using amount of the disintegrating agent is 15-30 percent of the total weight of a tablet; the using amount of the diluent is 0-20 percent of the total weight of the tablet; the using amount of the lubricating agent is 0.1-2 percent of the total weight of the tablet; and the using amount of the flow aid is 0.1-2 percent of the total weight of the tablet. Due to the adoption of the medicinal preparation prepared in the invention, the defects of poor flowability of a crystal form a and difficulty in preparing a solid preparation can be well overcome, the prepared medicinal preparation is dissolved quickly, and the crystal form does not change in preparing and storing processes.

Description

Technical field: [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a pharmaceutical preparation for treating chronic myeloid leukemia imatinib mesylate, more specifically a pharmaceutical preparation containing α crystal form imatinib mesylate. technical background [0002] The present invention relates to a kind of tyrosine kinase inhibitor imatinib mesylate (Imatinib mesylate), which is used for the treatment of chronic myelogenous leukemia (CML) patients in blast phase, accelerated phase or chronic phase after alpha-interferon treatment failure . Chemical name: 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[4-(3-pyridyl)-2-pyrimidinyl]amino] Phenyl]benzamide methanesulfonate; [0003] This compound has the following structural formula: [0004] [0005] Chronic myelogenous leukemia (CML) accounts for approximately 20% of all types of leukemia and is diagnosed by detecting the presence or absence of the Philadelphia...

Claims

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Application Information

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IPC IPC(8): A61K31/506A61K9/20A61K9/48A61K47/04A61K47/12A61K47/36A61K47/38A61K47/10A61P35/02
Inventor 姜锋崔媛刘衡王祎张克星
Owner TIANJIN TAIPU PHARMA SCI & TECH DEV
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