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Nimesulide preparation and preparation method thereof

A preparation and disintegrant technology, applied in the field of nimesulide preparations and preparations thereof, can solve the problems of reducing the drug efficacy of the preparation, restricting the application, etc., and achieve the effects of high drying efficiency, reducing the quality change of the preparation, and fast dissolution rate

Active Publication Date: 2018-10-16
湖北舒邦药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because nimesulide will undergo crystal transformation in ethanol solution, the drug efficacy of the preparation obtained by the above scheme is reduced, which limits its application

Method used

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  • Nimesulide preparation and preparation method thereof
  • Nimesulide preparation and preparation method thereof
  • Nimesulide preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065]

[0066] Preparation process: Mix nimesulide raw materials, lactose, microcrystalline cellulose, sodium lauryl sulfate, and sodium carboxymethyl starch internally, add to a wet granulator and stir for 4 minutes to make the mixture even, add hydroxypropyl fiber Stir the plain aqueous solution, 25HZ shear granulation for 4min, wet granules with 24 mesh sieve, granulate with 40 mesh sieve after drying at 60-65℃ until the water content is less than 4.0%, and mix with lubricant and external disintegrating agent, according to the theory Tablet weight for tablet compression. The content uniformity and friability of the plain tablets passed the test.

[0067] The dissolution results of this preparation are shown in Table 1 below.

[0068] Table 1 Example 1 Nimesulide Dispersible Tablets Dissolution Curve Results in Each Medium

[0069] Dissolution medium

Embodiment 2

[0071]

[0072] Preparation process: Mix nimesulide raw materials, lactose, microcrystalline cellulose, sodium lauryl sulfate, and sodium carboxymethyl starch internally, add to a wet granulator and stir for 4 minutes to make the mixture even, add hydroxypropyl fiber Stir the plain aqueous solution, 25HZ shear granulation for 4min, wet granules with 24 mesh sieve, granulate with 40 mesh sieve after drying at 60-65℃ until the water content is less than 4.0%, and mix with lubricant and external disintegrating agent, according to the theory Tablet weight for tablet compression. The content uniformity and friability of the plain tablets passed the test.

[0073] The dissolution results of this formulation are shown in Table 2 below.

[0074] Dissolution curve result in each medium of table 2 embodiment 2 nimesulide dispersible tablet

[0075] Dissolution medium

Embodiment 3

[0077]

[0078]

[0079] Preparation process: Mix nimesulide raw materials, lactose, microcrystalline cellulose, sodium lauryl sulfate, and sodium carboxymethyl starch internally, add to a wet granulator and stir for 4 minutes to make the mixture even, add hydroxypropyl fiber Stir the plain aqueous solution, 25HZ shear granulation for 4min, wet granules with 24 mesh sieve, dry at 80-95°C until the water content is less than 4.0%, and then granulate with 40 mesh sieve and mix with lubricant and external disintegrant, according to the theory Tablet weight for tablet compression. The content uniformity and friability of the plain tablets passed the test.

[0080] The dissolution results of this formulation are shown in Table 3 below.

[0081] Dissolution curve result in each medium of table 3 embodiment 3 nimesulide dispersible tablet

[0082] Dissolution medium

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PUM

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Abstract

The invention provides a nimesulide preparation and a preparation method thereof. The nimesulide preparation is mainly prepared from the following components in percentage by weight by wet granulation: 19.0%-28.0% of nimesulide, 0.07%-0.50% of a surfactant, 1.0%-2.0% of a binder, 4.0%-9.0% of a disintegrant, 30.0%-70.0% of filler, 0.5%-1.2% of a lubricant and the balance of water. The nimesulide preparation is prepared from water as a wetting agent by granulation, possible crystal transformation and toxic and side effects are avoided, safety and efficacy of the preparation are guaranteed, andfaster dissolution is realized.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a nimesulide preparation and a preparation method thereof. Background technique [0002] Nimesulide is a patented product of Helsinn in Switzerland. It was first launched in Italy in 1985 and has been used in more than 50 countries. Its market size exceeds US$1 billion, including France, Portugal, Greece, Switzerland, Belgium, In Russia, Thailand and Brazil, tablets are marketed under the trade names Aulin and Mesulid, with a strength of 100 mg (RLD). Nimesulide has never passed (FDA) evaluation in the United States, and it has not been marketed. The trade names of Nimesulide are Aulin and Mesulid. It is a non-steroidal anti-inflammatory drug that can selectively inhibit cyclooxygenase II, so it has significant anti-inflammatory, analgesic and antipyretic effects. A large number of clinical literatures at home and abroad show that compared with ibuprofen and acetaminophen, nimesulide h...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/18A61P29/00
CPCA61K9/2054A61K9/2059A61K9/2095A61K31/18A61P29/00
Inventor 黄晶杨刚李守明王洪萍马明为
Owner 湖北舒邦药业有限公司
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