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Stable montelukast sodium tablet and preparation method thereof

A stabilizer and stabilizing technology, applied in the field of pharmaceutical compositions containing montelukast or its salts, can solve the problems of wasteful tailings, poor friability, poor lubricity, etc.

Inactive Publication Date: 2013-03-20
NANJING REAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the requirements for dry granulation equipment are relatively high. In addition, there are more fine powders and more waste tailings. At the same time, due to poor lubricity, it is easy to interfere during tablet compression, resulting in pitting on one side and poor friability.
And because there is no stabilizer added, the increase of impurities is more obvious during long-term and accelerated storage

Method used

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  • Stable montelukast sodium tablet and preparation method thereof
  • Stable montelukast sodium tablet and preparation method thereof
  • Stable montelukast sodium tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029]

[0030] Preparation process: Montelukast sodium is passed through a 100-mesh sieve, iron oxide red is passed through a 80-mesh sieve, the prescribed amount of iron oxide red, microcrystalline cellulose, sodium carboxymethyl starch, and VA64 are weighed and mixed evenly, and then the prescribed amount is Montelukast sodium and the above mixture were added in equal amounts for 3 times and mixed evenly, passed through an 80-mesh sieve for dry granulation, plus the prescribed amount of micropowder silica gel and zinc stearate, mixed evenly, compressed into tablets, and coated.

[0031] Example 1

[0032]

[0033] Preparation Process

[0034] (1) Montelukast sodium is passed through a 100-mesh sieve, and magnesium metasilicate is passed through an 80-mesh sieve for subsequent use;

[0035] (2) Adhesive configuration: take the prescription amount of povidone K30, dissolve it in 40% ethanol solution, and prepare a 40% ethanol solution of 5% povidone K30;

[0036] (3) ...

Embodiment 2

[0042]

[0043] Preparation Process

[0044] (1) Montelukast sodium is passed through a 100-mesh sieve, and magnesium metasilicate is passed through an 80-mesh sieve for subsequent use;

[0045] (2) Adhesive configuration: take the prescription amount of povidone K30, dissolve it in 40% ethanol solution, and prepare a 40% ethanol solution of 5% povidone K30;

[0046] (3) Take the sieved montelukast sodium and magnesium aluminosilicate, and mix them evenly; then weigh the microcrystalline cellulose, lactose, and croscarmellose sodium of the prescribed amount and mix them with the above mixed powder Uniform;

[0047] (4) Add adhesive to prepare soft material in (3) mixed powder, cross 18 mesh sieves to prepare wet granules;

[0048] (5) Start the blower to suck the material into the F-200B fluidized dryer. The air inlet temperature is set at 60°C±5°C, the outlet air temperature is set at 50°C±5°C, the material temperature is ≤55°C, and the drying time is about 25 minutes; ...

Embodiment 3

[0052]

[0053] Preparation Process

[0054] (1) Montelukast sodium is passed through a 100-mesh sieve, and magnesium metasilicate is passed through an 80-mesh sieve for subsequent use;

[0055] (2) Weigh the sieved montelukast sodium and magnesium aluminosilicate, and mix them evenly; then weigh the prescribed amount of microcrystalline cellulose, lactose, and croscarmellose sodium to mix with the above mixed powder Uniform; add magnesium stearate with general prescription quantity and mix with the above-mentioned mixed powder;

[0056] (3) Start the dry granulator, adjust the distance between the rollers to 0.5 mm, the feeding speed to 42 revolutions / min, the speed of the pressing wheel to 5 revolutions / min, and the screen mesh to be 10-18 mesh, and pour the above materials into the feeding hopper , receive material from the outlet.

[0057] (4) adding the magnesium stearate compressed tablet of prescription quantity;

[0058] (5) Coating, adopt Opadry red coating powd...

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PUM

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Abstract

The invention relates to a stable pharmaceutical composition containing montelukast or salt of the montelukast and a method for preparing the composition. The montelukast sodium is easily affected by moist heat and light and degraded into sulfoxide and cis-isomer, so as to become a problem for development of a pharmaceutical preparation. A stabilizer is added to the stable montelukast sodium tablet disclosed by the invention to coexist with the montelukast sodium. Therefore, increase of the sulfoxide and the cis-isomer can be restrained to the maximal extent.

Description

technical field [0001] The present invention relates to stable pharmaceutical compositions comprising montelukast or salts thereof and processes for the preparation of such compositions. Preferably, the salt is a sodium salt. In particular, the present invention comprises a film-coated tablet in the presence of montelukast sodium and a stabilizer. Background technique [0002] Asthma is a chronic inflammatory disease characterized by tracheal hyperresponsiveness and reversible airway obstruction. Leukotrienes are one of the important mediators of bronchial asthma. They play a key role in the occurrence and development of asthma. Studies have shown that the response it causes is similar to the pathological changes of asthma in vivo or in vitro. Or in the stable period, its level is higher than that of normal people. Leukotriene receptor antagonists have become a new approach in the treatment of asthma. [0003] Montelukast is a highly specific cysteinyl leukotriene recept...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/47A61K47/02A61K47/10A61K47/18A61P11/06
Inventor 时文祥李玉凤赵静相文杰
Owner NANJING REAL PHARMA
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