Preparation method of methylsulfonic acid imatinib tablet

Abstract

The invention discloses a preparation method of methylsulfonic acid imatinib tablet. The invention takes organic solvent or organic solution with volume concentration bigger than 70% as pelletization solution, and the weight of water-insoluble filling agent in the tablet accounts for less than 20% of the total weight of the tablet. The invention has advantages of simple technical process, high yield and good dissolution of a product.

Description

technical field The invention relates to a preparation method of a tablet containing imatinib mesylate. Background technique Imatinib mesylate, developed by Novartis, is the world's first approved inhibitor of tumorigenesis-related signal transduction. Its chemical name is: 4-[(4-methyl-1-piperazine)methyl]-N-[4-methyl-3-[[4-(3-pyridine)-2-pyrimidine]amino]benzene base]-aniline methanesulfonate. Molecular formula: C 29 h 31 N 7 O·CH 4 SO 3 Molecular weight: 589.7 The simplified structure is: WO2009 / 042803 discloses the technology of producing imatinib mesylate tablets by dry granulation process, and the ratio of its raw material drug is 23-29%. EP1762230B1 protects the process of producing coated tablets, mainly dry granulation process, and the amount of API is between 25-80%. The production of imatinib mesylate tablets by dry granulation has certain defects in commercial production. Relatively speaking, the amount of dust generated in the dry granulation pr...

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Problems solved by technology

In addition, it was found that there was a problem of low dissolution

This may be due to the accumulation of insoluble excipients such as microcrystalline cellulose making it difficult to dissolve the raw material

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