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Roflumilast tablet and preparation method thereof

A technology of roflumilast tablets and roflumilast, which is applied in the directions of pill delivery, respiratory diseases, active ingredients of heterocyclic compounds, etc., can solve the problems of slow drug speed, undisclosed, slow disintegration of tablets, etc.

Inactive Publication Date: 2014-11-26
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

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034]

[0035]

[0036] Preparation method: Grind the raw material of roflumilast with a jet mill, weigh 1000 tablets of the raw material of roflumilast in the prescription amount, and set aside; adopt the method of increasing the amount in equal amounts, first mix the raw material of roflumilast with the prescription amount The croscarmellose sodium is fully mixed, and then fully mixed with the prescribed amount of microcrystalline cellulose, direct-pressed lactose, and magnesium stearate in turn; the mixed powder is tested for bulk density and angle of repose, and the compressive strength is converted according to the content. Tablet weight, perform tablet compression, adjust the hardness of the tablet to 2-3kg, and the difference in filling capacity is ±5.0%.

Embodiment 2

[0038]

[0039] Preparation method: Grind the raw material of roflumilast with a jet mill, weigh 1000 tablets of the raw material of roflumilast in the prescription amount, and set aside; adopt the method of increasing the amount in equal amounts, first mix the raw material of roflumilast with the prescription amount The croscarmellose sodium is fully mixed, and then fully mixed with the prescribed amount of pregelatinized starch, microcrystalline cellulose, direct-pressed lactose, and magnesium stearate in turn; after the content of the mixed material is tested, it is converted according to the content The weight of the tablet should be pressed, and the tablet should be pressed to adjust the hardness of the tablet to 2-3kg, and the difference in the filling volume should be ±5.0%.

Embodiment 3

[0041]

[0042]

[0043] Preparation method: Grind the raw material of roflumilast with a jet mill, weigh 1000 tablets of the raw material of roflumilast in the prescription amount, and set aside; adopt the method of increasing the amount in equal amounts, first mix the raw material of roflumilast with the prescription amount Sodium carboxymethyl starch is fully mixed, and then fully mixed with pregelatinized starch, microcrystalline cellulose, direct-pressed lactose, and magnesium stearate in sequence; after the mixed powder detects the angle of repose and bulk density content, according to The weight of the tablet should be converted into the content, and the tablet should be pressed to adjust the hardness of the tablet to 2-3kg, and the difference in the filling amount should be ±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 in particular relates to a chronic obstructive pulmonary disease (COPD) inhibitor roflumilast tablet and a preparation method thereof. Background technique [0002] Roflumilast (Roflumilast) is a new type of oral drug developed by Nycomed of Germany for the treatment of asthma and chronic obstructive pulmonary disease. It was approved by the US FDA in 2011 for the treatment of chronic obstructive pulmonary disease. The listed dosage form is a tablet. 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, the structural formula is as follows: [0004] [0005] Roflumilast and its active metabolite roflumilast nitrox in vivo are selective inhibitors of phosphodiesterase type 4...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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