Apremilast tablets and preparation method thereof

Abstract

The invention discloses apremilast tablets. Plain tablets of the tablets comprise active components and an excipient, wherein the mass of the active components is 5%-15% of that of the plain tablets,the excipient comprises an excipient A, the excipient A is selected from one or a mixture of more of lactose, microcrystalline cellulose, Ludipress and Ludipress LCE, the mass of the excipient A is 80%-92% of that of the plain tablets, and the excipient A is further selected from 85%-90%. A preparation method of the apremilast tablets comprises the following steps of crushing the active componentsfor standby application, wherein the size distribution d(0.9) of the crushed active components is smaller than or equal to 15.0 [mu]m; screening the excipient for standby application; screening the active components and the excipient, and performing uniform mixing; and performing tabletting and coating. According to the apremilast tablets and the preparation method thereof disclosed by the invention, the dissolution rate of the apremilast in the tablets is greatly increased; and besides, the preparation technology is simple, controllable, environmentally-friendly and sustainable, the production cost is low, the production efficiency is high, and the apremilast tablets and the preparation method are suitable for large-scale industrialization big production.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an apremilast tablet and a preparation method thereof. Background technique [0002] Apremilast, the English name is Apremilast, the chemical name is S-(2-(1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl)-4-acetylamino Isoindoline-1,3-dione, molecular formula C 22 h 24 N 2 o 7 S, the molecular weight is 460.50, the chemical structure formula is as follows: [0003] [0004] Apremilast is a small molecule phosphodiesterase-4 (PDE-4) inhibitor, which can regulate the action of intracellular pro-inflammatory and anti-inflammatory factors, reduce joint swelling and improve the physiological function of joint parts. Apremilast was developed by Celgene Corporation of the United States and was initially approved for marketing in the United States in March 2014. The product name is For the treatment of adult patients with active psoriatic arthritis. Celgene submitted another applica...

AI Technical Summary

Problems solved by technology

[0007] In the research work of Apremilast, the inventor unexpectedly discovered a kind of Apremilast oral tablet and its preparation method, which can effectively solve the insoluble problem of Apremilast and its inhydrochloric acid solution (pH1.0) problems such as rapid degradation, poor oral absorption, complex operation process, etc.

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