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Large-scale preparation technology for high-purity mesalazine enteric-coated sustained-release tablet preparations

A technology of mesalazine and preparation technology, which is applied in the field of preparation of chemical drugs, and can solve problems such as physical health damage and ineffective improvement of treatment effect

Pending Publication Date: 2021-04-20
南京森博医药研发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above methods are all prepared by enteric-coated technology and tablet-compressing technology, supplemented with other substances, the obtained enteric-coated sustained-release tablets are conventional drugs, and the improvement of therapeutic effect is not obvious
In addition, the povidone (PVP) used as a binder is a type 3 carcinogen, and long-term use will cause damage to health

Method used

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  • Large-scale preparation technology for high-purity mesalazine enteric-coated sustained-release tablet preparations
  • Large-scale preparation technology for high-purity mesalazine enteric-coated sustained-release tablet preparations

Examples

Experimental program
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Effect test

Embodiment 1

[0023] In parts by weight, dissolve 100 parts of polyglutamic acid in 300 parts of water, add N-hydroxysuccinimide NHS solution and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide The hydrochloride EDC solution (volume ratio of 1:1) was reacted at room temperature for 6 h to obtain an activated polyglutamic acid solution. Then the activated polyamino acid solution was added with a mass ratio of 1:0.3 ethylene glycol dimethacrylate and azobisisobutyronitrile, mixed uniformly, and reacted at 3 °C for 0.5 h, and then the product was mixed with 300 parts of polyethylene The aqueous alcohol solution (mass fraction of 25 wt %) was mixed, and the reaction was stirred at 30° C. for 2 h to obtain a polyvinyl alcohol-polyglutamic acid copolymer. Under stirring, slowly add 50 parts of mesalazine and 200 parts of polyvinyl alcohol-polyglutamic acid copolymer into the rapid wet mixing granulator, add 15 parts of sodium alginate immediately after adding, keep stirring, until A suitable soft ...

Embodiment 2

[0025] Dissolve 100 parts of polyglutamic acid in 300 parts of water, add N-hydroxysuccinimide NHS solution and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC solution ( The volume ratio is 1:2), and the reaction is carried out at room temperature for 4 h to obtain an activated polyglutamic acid solution. Then add ethylene glycol dimethacrylate and azobisisobutyronitrile in a mass ratio of 1:0.3 to the activated polyamino acid solution, mix them evenly, and react at 0 °C for 1 h, and then mix the product with 400 parts of polyvinyl alcohol. The aqueous solution (mass fraction of 30 wt %) was mixed, and the reaction was stirred at 40° C. for 3 h to obtain a polyvinyl alcohol-polyglutamic acid copolymer. Under stirring, slowly add 50 parts of mesalazine and 250 parts of polyvinyl alcohol-polyglutamic acid copolymer into the rapid wet mixing granulator, and immediately add 5 parts of hydroxypropyl methylcellulose after adding, Keep stirring until a suitable soft...

Embodiment 3

[0027]Dissolve 100 parts of polyglutamic acid in 200 parts of water, add N-hydroxysuccinimide NHS solution and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC solution ( The volume ratio is 1:2), and the reaction is carried out at room temperature for 8 hours to obtain an activated polyglutamic acid solution. Then add ethylene glycol dimethacrylate and azobisisobutyronitrile in a mass ratio of 1:0.5 to the activated polyamino acid solution, mix them evenly, and react at 5°C for 0.5h, and then mix the product with 400 parts of polylactic acid. The aqueous solution (mass fraction of 20 wt %) was mixed, and the reaction was stirred at 35° C. for 2 h to obtain a polylactic acid-polyglutamic acid copolymer. Under stirring, slowly add 50 parts of mesalazine and 400 parts of polylactic acid-polyglutamic acid copolymer into the rapid wet mixing granulator, add 20 parts of agar immediately after adding, and keep stirring until a suitable Soft material; after the soft m...

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Abstract

The invention discloses a large-scale preparation technology for high-purity mesalazine enteric-coated sustained-release tablet preparations. The preparation technology includes the following steps: dissolving polyglutamic acid into water, adding an N-hydroxysuccinimide NHS solution and a 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC solution, and performing reaction for 4-8 h at room temperature so as to obtain an activated polyglutamic acid solution; adding a cross-linking agent and an initiator with the mass ratio being 1:(0.1-0.5) into the activated polyglutamic acid solution, performing reaction for 0.5-1 h at 0-5 DEG C after uniform mixing, then mixing the product and a water-soluble polymer solution, and performing stirring reaction for 1-3 h under 30-40 DEG C to obtain water-soluble polymer-polyglutamic acid copolymer; slowly adding mesalazine and the water-soluble polymer-polyglutamic acid copolymer into a granulating machine under stirring, then adding a thickening agent, and forming a suitable soft material through stirring; and preparing the soft material into dried granules, and obtaining the high-purity mesalazine enteric-coated sustained-release tablet preparations through tablet compressing and coating. The preparation technology is simple and suitable for commercial process.

Description

technical field [0001] The invention belongs to the technical field of chemical preparation, in particular to a large-scale preparation process of a high-purity mesalazine enteric-coated sustained-release tablet preparation. Background technique [0002] Ulcerative colitis (UC) is a chronic non-specific intestinal inflammation with unclear etiology. The lesions are mainly located in the mucosa and submucosa of the colorectum, and can form visible erosions and ulcers. The range of lesions mostly starts from the distal colon, develops reversibly to the proximal end, and even involves the whole colon and occasionally the terminal ileum, showing a continuous distribution. The incidence of the disease is high in Europe and the United States, and relatively low in Asian and African countries. In recent years, the number of reported cases in China has gradually increased, and the incidence of UC in my country has shown an upward trend. Because the etiology and pathogenesis of the ...

Claims

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Application Information

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IPC IPC(8): A61K9/32A61K31/606C08G81/02A61P1/00A61P1/04A61P29/00
Inventor 赵冰清骆晓群徐晶欧明月
Owner 南京森博医药研发有限公司
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