Imatinib mesylate gastric-soluble pellet tablet and preparation method thereof

Abstract

The invention discloses an imatinib mesylate pellet tablet and a preparation method thereof. The preparation method comprises the following steps: firstly, preparing a main drug, namely imatinib mesylate, into a gastric-soluble coating pellet by a fluidized bed coating process, and then mixing the coating pellet with a filling agent, a disintegrating agent, an adhesive, a plasticizing agent, a lubricating agent and the like to prepare the gastric-soluble tablet by a compressing dry granulation technology. The tablet can be directly swallowed and can be quickly disintegrated into pellets in water so as to be convenient for patients with dysphagia and especially children to take. The accurate dose of the tablet can be ensured, and the tablet can be taken safely and conveniently.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to a micropill, in particular to a stomach-soluble imatinib mesylate micropill and a preparation method thereof. Background technique [0002] Imatinib, whose chemical name is 4-(4-methylpiperazine-1-methyl)-N-[4-methyl-3-[4-(3-pyridyl)-amino]phenylpyrimidine ]-2-benzamide, the trade name is Gleevec. The drug is a small molecule tyrosine kinase inhibitor antineoplastic drug originally developed by Swiss Novartis. The breakthrough anti-tumor mechanism of imatinib allowed it to obtain express approval from the US FDA in May 2001 for the treatment of chronic myelogenous leukemia due to failure of α-interferon administration. Because the body absorbs its mesylate salt, imatinib mesylate, the drug is usually given orally as the mesylate salt. [0003] Imatinib mesylate is currently only available in tablets or capsules. The specifications of tablets are 100mg, 400mg, and the specifications of ca...

AI Technical Summary

Problems solved by technology

However, for children, the dose of the pill is relatively large, which is inconvenient to take

[0007] [CN101401797A] discloses a preparation method containing imatinib mesylate effervescent tablets, the dosage form can form a uniform solution in water, has a high degree of drug dispersion, fast onset speed, and high blood drug concentration; however Effervescent tablets need to be dissolved before taking, do not swallow

[0008] [CN101401795A] discloses a kind of imatinib mesylate orally disintegrating tablet, which disintegrates rapidly, takes effect quickly, and the drug is fully absorbed, and is suitable for use by patients who do not swallow; however, due to the disintegration of the drug in the oral cavity , even if flavoring agents are added, the bitterness of the drug itself cannot be completely covered, especially for children, the drug compliance is still poor

[0009] Similarly, a kind of imatinib mesylate chewable tablet invented by [CN101401794A] is similar to the above-mentioned orally disintegrating tablet, which cannot improve children’s medication compliance well.

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