Apremilast tablets and preparation method thereof

A special tablet and Aps technology, applied in the field of medicine, can solve the problems of insoluble, poor oral absorption, complicated operation process, etc., and achieve the effects of low production cost, increased dissolution rate, and simple and controllable preparation process.

Inactive Publication Date: 2019-12-10
CHENGDU BAIYU PHARMA CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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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 solv...

Method used

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  • Apremilast tablets and preparation method thereof
  • Apremilast tablets and preparation method thereof
  • Apremilast tablets and preparation method thereof

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preparation example Construction

[0037] The preparation technology of the Apremilast tablet of above embodiment 1~4 is as follows:

[0038] (1) The active ingredient of the medicine is pulverized by jet, and it is set aside;

[0039] (2) Excipient C is passed through a 40-mesh sieve, excipient A is passed through a 60-mesh sieve, and excipient B is passed through a 80-mesh sieve for subsequent use;

[0040] (3) Weigh excipient A and excipient C according to the prescription amount, sieve and mix them; weigh the API of the prescription amount, and mix them uniformly in the manner of equal increment;

[0041] (4) Weigh the excipient B of the prescribed amount and add it, mix evenly, and press the tablet with a shallow concave arc-shaped Φ6mm die;

[0042] (5) The Opadry is formulated into a solution with a solid content of 20.0 wt%, and coated, and the temperature of the air inlet is controlled at 40-60°C, and the temperature of the exhaust air is 35-45°C.

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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...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K31/4035A61P19/02A61P17/06
CPCA61K9/2054A61K9/2095A61K9/2866A61K31/4035A61P17/06A61P19/02
Inventor 周家友赖庆宽黄劲甘林建
Owner CHENGDU BAIYU PHARMA CO LTD
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