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Celecoxib composition and preparation method thereof

A technology for celecoxib and a composition, which is applied in the field of pharmaceutical preparations, can solve the problems of low dissolution rate and low bioavailability, and achieves the effects of high dissolution rate, improved dissolution rate and stable properties.

Inactive Publication Date: 2017-09-01
FUJIAN FUKANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to provide a celecoxib composition and a preparation method thereof, aiming at solving the problems of low dissolution rate and low bioavailability of celecoxib capsules in the prior art

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A celecoxib composition, consisting of the following components: celecoxib 100g, microcrystalline cellulose 15g, Tween-80 is 2g, sodium carboxymethyl starch 1g, povidone K30 is 2g, stearic acid Magnesium 0.8g.

[0028] The preparation method is:

[0029] 1) Weigh celecoxib, microcrystalline cellulose, Tween-80, sodium carboxymethyl starch, povidone K30 and magnesium stearate respectively, control the particle size of celecoxib at D90≤10μm, except Tween The auxiliary materials other than -80 are passed through a 60-80 mesh sieve and set aside;

[0030] 2) Add celecoxib, microcrystalline cellulose, sodium carboxymethyl starch, and povidone K30 into the wet granulator, pre-mix for 5 minutes, turn on the slow speed of stirring and the slow speed of the cutter, and slowly add Tween-80 The aqueous solution of the solution is wet granulated, granulated for 3 minutes;

[0031] 3) The prepared wet granules are sent to a drying oven for drying at a drying temperature of 60°C u...

Embodiment 2

[0036] A celecoxib composition, consisting of the following components: celecoxib 100g, microcrystalline cellulose 10g, starch 25g, Tween-80 is 4.1g, crospovidone 2g, croscarmellose Sodium 1.5, hypromellose 4g, magnesium stearate 3.5g.

[0037] The preparation method is:

[0038] 1) Weigh celecoxib, microcrystalline cellulose, starch, Tween-80, crospovidone, croscarmellose sodium, hypromellose, magnesium stearate, and celecoxib respectively The particle size of coxib is controlled at D90≤10μm, and the excipients except Tween-80 are passed through a 60-80 mesh sieve for later use;

[0039] 2) Add celecoxib, microcrystalline cellulose, starch, crospovidone, croscarmellose sodium, and hypromellose into the wet granulator in sequence, premix for 5 minutes, start stirring slowly Slow speed and cutter speed, slowly add Tween-80 aqueous solution for wet granulation, granulation for 4 minutes;

[0040] 3) The wet granules are sent to the drying oven for drying, the drying temperatu...

Embodiment 3

[0045] A celecoxib composition, consisting of the following ingredients: celecoxib 100g, lactose 24.9g, sodium lauryl sulfate 4.1g, croscarmellose sodium 1.4g, povidone K30 is 3.4 g, magnesium stearate is 1.4g.

[0046] The preparation method is:

[0047] 1) Weigh celecoxib, lactose, sodium lauryl sulfate, croscarmellose sodium, povidone K30, magnesium stearate, celecoxib particle size D90≤10μm, except twelve Auxiliary materials other than sodium alkyl sulfate are passed through a 60-80 mesh sieve and set aside;

[0048]2) Add celecoxib, lactose, croscarmellose sodium, and povidone K30 into the wet granulator in sequence, pre-mix for 5 minutes, turn on the slow speed of stirring and the slow speed of the cutter, and slowly add dodecane The aqueous solution of sodium sulfate was wet granulated, and the granulation was 6 minutes;

[0049] 3) The wet granules are sent to the drying oven for drying, the drying temperature is 58°C, and the moisture content of the granules is con...

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PUM

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Abstract

The invention discloses a celecoxib composition and a preparation method thereof. The celecoxib composition is prepared from the following components in parts by weight: 100 parts of celecoxib, 15 to 35 parts of filler, 2 to 4.1 parts of solubilizing agents, 1 to 3.5 parts of disintegrant, 2 to 4 parts of binder and 0.8 to 3.5 parts of lubricant. The preparation method comprises the steps: 1) weighing each component correspondingly; 2) adding the celecoxib, the filler, the disintegrant and the binder to a wet type granulator, premixing; and then slowly adding a solubilizing agent solution to perform wet granulation; 3) drying wet granules in a drying oven, keeping drying temperature to be 50 to 70 DEG C, controlling the water content of particle to be less than or equal to 3%; 4) granulating the dried particles, sending the particles into a mixer to mix with the lubricant; 5) testing the mixed particles, and filling the particles with capsules. The celecoxib composition provided by the invention has a high dissolution rate and a high bioavailability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a celecoxib composition and a preparation method thereof. Background technique [0002] Celecoxib (Celecoxib), has a unique mechanism of action that specifically inhibits COX-2, the chemical name is 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1 hydrogen-1 -pyrazol-1-yl]benzenesulfonamide, whose molecular formula is C 17 h 14 f 3 N 3 o 2 S, with a molecular weight of 381.38; Celecoxib is the first specific cyclooxygenase-2 (COX-2) inhibitor jointly developed by Searle and Pfizer. Celecoxib capsules were first released in January 1999 Approved for marketing in the United States, it is used to relieve arthritis-related pain. It is currently the most prescribed non-steroidal anti-inflammatory analgesic in the world. [0003] Celecoxib is a white to off-white crystalline powder, which is almost insoluble in water. The solubility in water at 25°C is 0.007m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K47/38A61K47/36A61K47/26A61K31/635A61P29/00
Inventor 郑志华
Owner FUJIAN FUKANG PHARMA
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