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Pharmaceutical composition containing roflumilast

A technology of roflumilast and composition, which is applied in the field of pharmacy, can solve problems such as complicated operation technology, and achieve the effect of simple operation

Inactive Publication Date: 2012-08-08
BEIJING WANQUAN SUNSHINE MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the operation technique is more complex

Method used

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  • Pharmaceutical composition containing roflumilast

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Weight ratio based on the tablet containing 0.5 mg roflumilast

[0024] 1. Roflumilast 0.76%

[0025] 2. Lactose 69.05%

[0026] 3. Corn starch 20.61%

[0027] 4. Crospovidone 7.49%

[0028] 5. Magnesium stearate 2.09%

[0029] Total 100%

[0030] Preparation Process:

[0031] Co-micronize the active ingredient roflumilast and part of lactose in the prescription, control the particle size of 90% volume or more particles in the range of 10-20um, pass all the excipients through 100 mesh respectively, and mix the micronized product with the remaining Measure lactose, corn starch, and crospovidone and mix them evenly in equal amounts, add an appropriate amount of 5% PVP K90, make soft materials, squeeze and sieve through a 18-mesh sieve to granulate, and dry the wet granules at a constant temperature at 50 degrees After 3 hours, the dry granules were sieved with a 24-mesh sieve, added with additional magnesium stearate, and mixed evenly.

[0032] A rotary tablet ...

Embodiment 2

[0035] Based on the weight of the tablet containing 0.125 mg roflumilast

[0036] 1. Roflumilast 0.11%

[0037] 2. Corn starch 47.01%

[0038] 3. Mannitol 42.11%

[0039] 4. Sodium carboxymethyl starch (internal addition) 5.00%

[0040] 5. Menthol 0.87%

[0041] 6. Sodium carboxymethyl starch (additional) 2.83%

[0042] 7. Magnesium stearate 2.06%

[0043] Total 100%

[0044] Preparation Process:

[0045] The active ingredient roflumilast in the prescription is micronized, and the particle size of 90% of the volume or more particles is controlled in the range of 10-30um,

[0046] All the excipients were passed through 100 meshes respectively, and the micronized roflumilast, corn starch, mannitol, sodium carboxymethyl starch, and menthol were mixed evenly in equal increments, and an appropriate amount of 5% hypromellose was added. Base cellulose, made of soft material, squeezed through a 18-mesh sieve and sieved to granulate. The wet granules were dried at a consta...

Embodiment 3

[0050] Based on the weight of the tablet containing 0.25 mg roflumilast

[0051] 1. Roflumilast 0.76%

[0052] 2. Corn starch 67.86%

[0053] 3. Sorbitol 22.14%

[0054] 4. Low-substituted hydroxypropyl cellulose 6.95%

[0055] 5. Magnesium stearate 2.29%g

[0056] Total 100%

[0057] Preparation Process:

[0058] The active ingredient roflumilast in the prescription is micronized, and the particle size of 90% of the volume or more particles is controlled within 50um, and all excipients are passed through 100 mesh respectively. Starch, sorbitol, and low-substituted hydroxypropyl cellulose are mixed uniformly by equal addition method, and an appropriate amount of 5% polyvinyl alcohol is added to make a soft material, which is extruded and sieved through a 18-mesh sieve to granulate, and the wet granules are placed at 50 degrees. Dry at constant temperature for 3 hours, sieve the dry granules through a 24-mesh sieve, add additional magnesium stearate, and mix well....

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Abstract

The invention relates to a pharmaceutical composition containing roflumilast. The pharmaceutical composition containing roflumilast has good dissolution effects and comprises components of roflumilast, water-soluble excipients and water-soluble polymer adhesives, wherein roflumilast is subjected to micronization so that 90% or more by volume of roflumilast particles have particle sizes of 5 to 50 microns and preferably have particle sizes of 10 to 20 microns. The pharmaceutical composition containing roflumilast has good dissolution effects so that the bioavailability of the pharmaceutical composition containing roflumilast is improved effectively.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and describes the preparation of a pharmaceutical preparation whose active ingredient is roflumilast. Roflumilast is used as an active ingredient in oral solid dosage form for the treatment of asthma or airway obstructive diseases. The invention additionally relates to a process for the production of this dosage form. Background technique [0002] Roflumilast N-(3,5-dichloro-pyridin-4-yl)-3-cyclopropylmethoxy-4-difluoromethoxybenzamide is a cyclic nucleotide phosphodiesterase ( A type of PDE) inhibitor (especially type 4). Cyclic nucleotide phosphodiesterase (PDE) inhibitors are currently the most attractive new generation of active ingredients for the treatment of inflammatory diseases (e.g., COPD = chronic obstructive pulmonary disease), so in aviation There are many applications in the company. Some PDE 4 inhibitors are currently undergoing further clinical trials. Such compounds with be...

Claims

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Application Information

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IPC IPC(8): A61K31/44A61K47/36A61P29/00
Inventor 张莹郭夏宋雪梅
Owner BEIJING WANQUAN SUNSHINE MEDICAL TECH CO LTD
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