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Diacerein composition with good leaching property, and preparation and use thereof

A technology of diacerein and composition, applied in the field of diacerein composition, can solve problems such as affecting the storage stability of the composition, increase in impurity content, etc., and achieve excellent dissolution performance, effective therapeutic concentration, and obvious clinical advantages. Effect

Inactive Publication Date: 2012-02-29
安士制药(中山)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In these preparations, because the corresponding composition contains polyoxyethylene sorbitan fatty acid ester or sodium lauryl sulfate, but as a component, it will affect the storage stability of the composition and increase the impurity content
There are no reports of better dissolution, stable diacerein tablets, dispersible tablets and hard capsules

Method used

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  • Diacerein composition with good leaching property, and preparation and use thereof
  • Diacerein composition with good leaching property, and preparation and use thereof
  • Diacerein composition with good leaching property, and preparation and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Take 50g of diacerein, 15g of starch, 30g of microcrystalline cellulose, 5g of sodium carboxymethyl starch and 1g of polyethylene glycol 6000, and pass through a 100-200 mesh sieve respectively, and take the sieved diacerein , starch, microcrystalline cellulose, sodium carboxymethyl starch, mixed evenly, made soft material with 5% povidone K-30 ethanol aqueous solution, granulated through 20 mesh sieve, dried at 45-60°C, passed 20 Mesh sieve for granulation, add polyethylene glycol 6000, mix evenly, measure the content of granules, press into tablets, the hardness is 5-7kgf, pack and inspect to obtain the finished product.

Embodiment 2

[0035] Example 2 Take 50g of diacerein, 45g of microcrystalline cellulose, 1g of sodium carboxymethyl starch, 5g of cross-linked polyvinylpyrrolidone and 1g of polyethylene glycol 4000, pass through 100-200 mesh sieves respectively, and take the sieved Diacerein, starch, microcrystalline cellulose, cross-linked polyvinylpyrrolidone, mix uniformly, make soft material with the ethanol aqueous liquid (50%) of 5% povidone K-30, cross 18 mesh sieves and granulate, Dry at 45-60°C, pass through a 14-mesh sieve for granulation, add polyethylene glycol 4000, mix evenly, measure the content of the granules, press into tablets, the hardness is 5-7kgf, pack and inspect to obtain the finished product.

Embodiment 3

[0036]Example 3 Take 50g of diacerein, 20g of starch, 25g of microcrystalline cellulose, 3g of low-substituted hydroxypropyl cellulose, 2g of sodium carboxymethyl starch and 1g of polyethylene glycol 6000, and pass through 100-200 mesh sieves respectively. Get sieved diacerein, starch, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, mix well, make soft material with 5% ethanol water (50%) of povidone K-30, Pass through a 24-mesh sieve to granulate, dry at 45-60°C, pass through a 24-mesh sieve for granulation, add polyethylene glycol 6000, mix evenly, measure the content of the granules, press into tablets, the hardness is 5-7kgf, pack and inspect to obtain the finished product.

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PUM

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Abstract

The invention relates to a diacerein composition with good leaching property, and preparation and a use thereof. The diacerein composition consists of diacerein and pharmaceutically acceptable adjuvants. The pharmaceutically acceptable adjuvants are selected from one or more from starch, microcrystalline cellulose, lactose, a disintegrating agent, a lubricant, an edulcorant and an adhesive. The diacerein composition quickly enters a blood circulation system more easily than an imported diacerein capsule, has better storage stability and is suitable for application to preparing drugs for preventing and treating arthritis, nephritis, glomerulonephritis and psoriasis as well as an interleukin-1 inhibitor.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to provide a diacerein composition with excellent dissolution performance, its preparation and application. Background technique [0002] Diacerein is a new interleukin (IL-1) inhibitor. Its mechanism of action (1) inhibits the activity of IL-1; (2) inhibits the synthesis of IL-1 in synovial tissue; (3) inhibits the expression of IL-1 receptor in chondrocytes; (4) inhibits collagenase and matrix dissolution (5) Promote the synthesis of collagen and amino polysaccharides; (6) Inhibit the chemotaxis of leukocytes and stabilize lysosomes. [0003] Clinical studies have shown that diacerein can significantly relieve symptoms and effectively modify the structure, and is a slow-acting drug that changes the symptoms and condition of osteoarthritis. All relevant trials have shown that diacerein can significantly improve the joint function of patients with osteoarthritis, delay the course...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/222A61K47/36A61K47/38A61K47/34A61K9/20A61K9/48A61P19/02A61P13/12A61P17/06A61K47/10
Inventor 刘力陈祺吴志刚戴静吕莹刘珍
Owner 安士制药(中山)有限公司
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