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Arformoterol tartrate orally disintegrating tablet and preparation method thereof

A technology of tartaric acid and orally disintegrating tablets, applied in the field of medicine, can solve the problems of low content uniformity, poor fluidity, and low deposition of effective parts

Pending Publication Date: 2022-03-18
BEIJING WANQUAN SUNSHINE MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, at present, the inhalation powder mist made of arformoterol tartrate into a compound preparation has poor fluidity, high hygroscopicity, low content uniformity, and low deposition of effective parts, which is not conducive to chronic bronchitis, asthmatic bronchitis, and emphysema. Treatment of dyspnea caused by airway obstructive pulmonary disease

Method used

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  • Arformoterol tartrate orally disintegrating tablet and preparation method thereof
  • Arformoterol tartrate orally disintegrating tablet and preparation method thereof
  • Arformoterol tartrate orally disintegrating tablet and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019]

[0020] Preparation Process:

[0021] 1) Arformoterol tartrate is pulverized and pretreated, and the particle size is 60 μm.

[0022] 2) Pass mannitol 100SD, microcrystalline cellulose PH101, crospovidone and acesulfame potassium through a 60-mesh sieve and mix for 3 times.

[0023] 3) Use purified water as a wetting agent to make a soft material, and granulate with a 30-mesh nylon sieve.

[0024] 4) Dry at 50°C until the moisture content of the granules is less than 3%, and sieve the granules with a 30-mesh steel sieve.

[0025] 5) To calculate the yield of the granulated granules, first add croscarmellose sodium, acesulfame potassium, menthol, and silicon dioxide and mix for 3 minutes. After mixing evenly, add magnesium stearate and mix for 1 minute.

[0026] 6) Use a φ7mm flat punch to press the tablet, the tablet weight is 150mg, the difference in the tablet is ±5%, and the hardness is 20-40N.

Embodiment 2

[0028]

[0029] Preparation Process:

[0030] 1) Arformoterol tartrate is pulverized and pretreated, and the particle size is 10 μm.

[0031] 2) Pass mannitol 100SD, microcrystalline cellulose PH101, crospovidone and acesulfame potassium through a 60-mesh sieve and mix for 3 times.

[0032] 3) Use purified water as a wetting agent to make a soft material, and granulate with a 30-mesh nylon sieve.

[0033] 4) Dry at 50°C until the moisture content of the granules is less than 3%, and sieve the granules with a 30-mesh steel sieve.

[0034] 5) To calculate the yield of the granulated granules, first add croscarmellose sodium, acesulfame potassium, menthol, and silicon dioxide and mix for 3 minutes. After mixing evenly, add magnesium stearate and mix for 1 minute.

[0035] 6) Use a φ7mm flat punch to press the tablet, the tablet weight is 150mg, the difference in the tablet is ±5%, and the hardness is 20-40N.

Embodiment 3

[0037]

[0038] Preparation Process:

[0039] 1) Arformoterol tartrate is pulverized and pretreated, and the particle size is 80 μm.

[0040] 2) Pass mannitol 100SD, microcrystalline cellulose PH101, crospovidone and acesulfame potassium through a 60-mesh sieve and mix for 3 times.

[0041] 3) Use purified water as a wetting agent to make a soft material, and granulate with a 30-mesh nylon sieve.

[0042] 4) Dry at 50°C until the moisture content of the granules is less than 3%, and sieve the granules with a 30-mesh steel sieve.

[0043] 5) To calculate the yield of the granulated granules, first add croscarmellose sodium, acesulfame potassium, menthol, and silicon dioxide and mix for 3 minutes. After mixing evenly, add magnesium stearate and mix for 1 minute.

[0044] 6) Use a φ7mm flat punch to press the tablet, the tablet weight is 150mg, the difference in the tablet is ±5%, and the hardness is 20-40N.

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Abstract

The invention provides arformoterol tartrate orally disintegrating tablets and a preparation method thereof. The arformoterol tartrate orally disintegrating tablet takes arformoterol tartrate with the particle size of 20-60 microns as a main component, auxiliary materials comprise a filling agent, a disintegrating agent and the like, and the product is prepared by adopting a wet granulation technology. The orally disintegrating tablet provided by the invention has good taste and short disintegration time, can be rapidly disintegrated when meeting saliva without drinking water, is convenient to take, and is especially suitable for special patients with dysphagia such as old people, children, coma patients and the like. Meanwhile, the orally disintegrating tablet can be prepared by adopting common pressing equipment and a simple process, the preparation method is simple and convenient, the quality is easy to control, and the orally disintegrating tablet is suitable for industrial production.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an orally disintegrating arformoterol tartrate tablet and a preparation method thereof. Background technique [0002] Arformoterol tartrate, chemical name: N-[2-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methyl Ethyl] amino] ethyl] phenyl] formamide; it is the corresponding isomer of formoterol, it is a long-acting selective adrenergic β2 receptor hormone drug, and its efficacy is that of formoterol 2 times of the spin body, 1000 times of the (S, S) corresponding isomer, and arformoterol tartrate has no side effects of (S, S)-formoterol to strengthen the bronchoconstriction reaction caused by acetylcholine, which can activate adenosine in the body Acid cyclase This enzyme can convert ATP into cAMP. The increase of intracellular cAMP can relax bronchial smooth muscle and reduce the release of allergic mediators from cells, especially hypertrophic cells. Yu Zhi ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/167A61K47/38A61K47/32A61K47/26A61K47/22A61K47/10A61K47/04A61P11/08
CPCA61K9/0056A61K9/2054A61K9/2027A61K9/2018A61K9/2013A61K9/2009A61K31/167A61P11/08
Inventor 马建洋王宇杰郭夏
Owner BEIJING WANQUAN SUNSHINE MEDICAL TECH CO LTD