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Roflumilast tablet and preparation method thereof

A technology of roflumilast tablets and roflumilast, which is applied in the directions of pharmaceutical formulations, medical preparations of inactive ingredients, and pill delivery, etc., can solve the problems of undisclosed, slow drug speed, and slow tablet disintegration.

Inactive Publication Date: 2013-06-05
深圳万乐药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] CN102274222A discloses a highly bioavailable roflumilast pharmaceutical composition and a preparation method thereof. The composition consists of roflumilast, beta-cyclodextrin, lactose, microcrystalline cellulose, and magnesium stearate. Prepared by direct compression method, undisclosed and original research product Comparison of dissolution results
Tablets prepared by wet granulation were slower to disintegrate and release drug into the dissolution medium at a slower rate

Method used

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  • Roflumilast tablet and preparation method thereof
  • Roflumilast tablet and preparation method thereof
  • Roflumilast tablet and preparation method thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0034]

[0035]

[0036] Preparation method: pulverize the raw material of Roflumilast with a jet mill, weigh out 1000 tablets of the raw material of Roflumilast, and use them for later use; use the method of adding the same amount of the raw material of Roflumilast to the prescription amount. The croscarmellose sodium is thoroughly mixed, and then it is thoroughly mixed with the prescribed amount of microcrystalline cellulose, direct-pressed lactose, and magnesium stearate; the bulk density and angle of repose of the mixed powder are measured, and the pressure is converted according to the content For tablet weight, press the tablet to adjust the hardness of the tablet to 2~3kg, with a difference of ±5.0%.

Embodiment 2

[0038]

[0039] Preparation method: pulverize the raw material of Roflumilast with a jet mill, weigh out 1000 tablets of the raw material of Roflumilast, and reserve them for use; adopt the method of adding the same amount, first combine the raw material of Roflumilast with the prescription amount The croscarmellose sodium is thoroughly mixed, and then it is thoroughly mixed with the prescribed amount of pregelatinized starch, microcrystalline cellulose, direct-pressed lactose, and magnesium stearate; after the content of the mixed material is tested, the content is converted according to the content The tablet should be compressed, and the hardness of the tablet should be adjusted to 2~3kg, with a difference of ±5.0%.

Embodiment 3

[0041]

[0042]

[0043] Preparation method: pulverize the raw material of Roflumilast with a jet mill, weigh out 1000 tablets of the raw material of Roflumilast, and use them for later use; use the method of adding the same amount of the raw material of Roflumilast to the prescription amount. Sodium carboxymethyl starch is thoroughly mixed, and then it is thoroughly mixed with the prescribed amount of pregelatinized starch, microcrystalline cellulose, straight-pressed lactose, and magnesium stearate; after the mixed powder is tested for the angle of repose and bulk density content, according to The content should be converted into the weight of the tablet, and the tablet should be compressed to adjust the hardness of the tablet to 2~3kg, and the difference in the filling amount is ±5.0%.

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Abstract

The present invention provides a Roflumilast tablet and a preparation method of the Roflumilast tablet. The method adopts a direct powder tabletting method, production process is easy, production cycle is shortened, equipment cost and operation cost are reduced, the prepared and obtained Roflumilast tablet is good in appearance, technical process is smooth, the method possesses good operability, product dissolution rate is high, content uniformity is qualified, the Roflumilast tablet can achieve good bioavailability in human body, and therefore good curative effects is produced.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to a chronic obstructive pulmonary disease (COPD) inhibitor roflumilast tablet and a preparation method thereof. Background technique [0002] Roflumilast is a new oral drug developed by the German company Nycomed for the treatment of asthma and chronic obstructive pulmonary disease. It was approved by the U.S. FDA in 2011 for the treatment of chronic obstructive pulmonary disease. The marketed dosage form is tablets. Product name , The specification is 0.5mg. [0003] The chemical name of Roflumilast is 3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide, and the molecular formula is C 17 H 14 Cl 2 F 2 N 2 O 3 , Molecular weight: 403.207, structural formula is as follows: [0004] [0005] Roflumilast and its active metabolite roflumilast nitroxide are selective inhibitors of phosphodiesterase type 4 (PDE4). Cyclic nucleotides cAMP and cG...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/44A61K47/38A61P11/06A61P11/00
Inventor 林浩文张广明柏江涛梁胜群刘相男袁庆
Owner 深圳万乐药业有限公司
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