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Diacerein composition and preparing method thereof

A technology of diacetyl rhein and a composition is applied in the directions of pharmaceutical formulations, medical preparations with inactive ingredients, medical preparations containing active ingredients, etc. and other problems to achieve the effects of alleviating gastrointestinal toxicity, increasing transmembrane transport, and reducing the occurrence of diarrhea

Active Publication Date: 2014-12-10
上海慈瑞医药科技股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Diacetylrhein is extremely insoluble in water and acid, so it cannot be completely absorbed when administered orally. As a typical non-steroidal anti-inflammatory drug, this drug has certain gastrointestinal toxicity due to incomplete absorption
The CN102406635A patent describes cyclodextrins and derivatives of diacetylrhein compounds and their preparation methods, which reduce the toxic and side effects of medicines, but the above-mentioned method is complicated to operate, requires relatively high technical requirements for preparations in the production process, and has relatively high production costs. High, difficult to carry out industrialized mass production

Method used

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  • Diacerein composition and preparing method thereof
  • Diacerein composition and preparing method thereof
  • Diacerein composition and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] A diacetyl rhein composition is made from the following raw materials in parts by weight:

[0024]

[0025] The preparation method is as follows: weigh each raw material in proportion, pass each solid raw material through a 100-mesh sieve, and take diacetyl rhein, poloxamer, sodium benzoate, lactose, crospovidone, polyvinylpyrrolidone, silicon dioxide Mix evenly, then pour into a tank mixer, add purified water while stirring, make soft material, pass through a 40-mesh sieve to granulate, then dry the granules at 60°C for 2 hours, take out the granules, let cool to room temperature, and pass through a 40-mesh sieve For granulation, 1% magnesium stearate is added according to the calculation of the granulated granules for granule blending, and finally the blended granules are filled in capsules, blistered, packaged, and made into capsules.

Embodiment 2

[0027] A diacetyl rhein composition is made from the following raw materials in parts by weight:

[0028]

[0029] Its preparation method is:

[0030] Each raw material is weighed in proportion, and diacetyl rhein, poloxamer, and sodium benzoate are respectively sieved to 80 meshes. Dissolve polyvinylpyrrolidone in 10% ethanol solution. Using a boiling granulator, put diacetyl rhein, poloxamer, sodium benzoate, microcrystalline cellulose, and croscarmellose sodium into the boiling granulator and mix well, turn on the fan, and control the temperature of the air inlet At 70°C, spray 10% ethanol solution of polyvinylpyrrolidone into a boiling granulator for boiling granulation, dry at 60°C for 2 hours, pass the granules through a 60-mesh sieve, add PEG6000 to mix, fill capsules, and pack.

Embodiment 3

[0032] A diacetyl rhein composition is made from the following raw materials in parts by weight:

[0033]

[0034] Each raw material is weighed in proportion, the above-mentioned materials are directly mixed, and directly compressed into tablets by a dry tablet press machine, blistered and packaged.

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Abstract

The invention provides a diacerein composition and a preparing method thereof. The diacerein composition is characterized by being prepared from the following raw materials in parts by weight: 1 part of diacerein, 0.01-0.1 part of poloxamer, 0.001-0.1 part of sodium benzoate, 0.3-6 parts of a filler, 0-0.5 part of a disintegrant, 0.01-0.5 part of an adhesive, 0-0.8 part of a moistening agent and 0.01-0.5 part of a lubricant. The diacerein composition not only can improve the solubility and the bioavailability of medicine, but also can reduce side effect generated when a patient takes the medicine.

Description

technical field [0001] The invention relates to a diacetyl rhein composition and a preparation method thereof, belonging to the technical field of pharmacy. Background technique [0002] Diacetylrhein, chemical name 4,5-diacetyl-9,10-dihydro-9,10-dioxo-2-anthracene carboxylic acid, commonly known as diacerein, insoluble in water, acid and common solvents , Soluble in dimethyl sulfoxide and N, N-dimethylformamide, easy to decompose in case of lye. Diacetylrhein can induce cartilage formation, has analgesic, anti-inflammatory and antipyretic effects; it can inhibit the production of IL-1, matrix metalloproteinase (MMP), etc., but does not inhibit the synthesis of prostaglandins; it has the effect of delaying the disease process of osteoarthritis , for the treatment of osteoarthritis and related diseases. Mild diarrhea is the most common side effect of diacerein treatment (incidence rate is about 7%). It usually occurs within the first few days after treatment, and in most ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/222A61K47/34A61K47/38A61K47/36
Inventor 成永靖谭永琦许洁
Owner 上海慈瑞医药科技股份有限公司
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