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Mesalazine oral controlled release medicine composition

A technology for oral salazine tablets and compositions, which is applied in directions such as drug combinations, sugar-coated pills, and pharmaceutical formulations, can solve the problems of complex preparation process, high production cost, no sustained-release effect, etc., and achieves improved compliance, low cost, The effect of reducing the number of doses

Active Publication Date: 2010-06-09
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Asacol is coated with Eudragit S100 and taken orally 3-4 times a day without sustained-release effect; Pentasa is coated with ethyl cellulose and taken orally 3-4 times a day; Lialda is a sustained-release preparation of mesalamine using MMX technology, It only needs one time. It is characterized by the use of lipophilic and hydrophilic materials as the substrate, but the process requires the use of melt granulation. The preparation process is complicated, requiring special equipment for melt granulation, and the production cost is high.

Method used

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  • Mesalazine oral controlled release medicine composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Tablet prescription:

[0033] Mesalamine 1200g

[0034] Sodium Carboxymethyl Cellulose 96g

[0035] Sodium carboxymethyl starch 48g

[0036] Magnesium Stearate 13.4g

[0037]

[0038] 1000 pieces

[0039] The preparation process of the tablet core: mix mesalazine, carboxymethylcellulose sodium and carboxymethyl starch sodium evenly, add appropriate amount of distilled water, granulate and dry. Add magnesium stearate, mix uniformly, measure the granule content, compress into tablets, and the main ingredient content of each tablet is 1.2g.

[0040] Coating Solution Prescription:

[0041] Coating Material Weight

[0042] Eudragit S100 200g

[0043] Eudragit L100 100g

[0044] Triethyl citrate 60g

[0045] Talc powder 10g

[0046] Titanium dioxide 30g

[0047] Iron Oxide Red 30g

[0048] Ethanol 4750ml

[0049] water 250ml

[0050] Coating process: Prepare the above coating solution a...

Embodiment 2

[0052] Tablet core prescription

[0053] Mesalamine 1200g

[0054] Hypromellose K 100 80g

[0055] Sodium carboxymethyl starch 30g

[0056]

[0057] Magnesium Stearate 13.0g

[0058]

[0059] 1000 pieces

[0060] Tablet core preparation process: uniform mesalazine and hypromellose K100, add appropriate amount of distilled water, granulate, and dry. Add magnesium stearate, mix uniformly, measure the granule content, compress into tablets, and the main ingredient content of each tablet is 1.2g.

[0061] Coating Solution Prescription:

[0062] Coating Material Weight

[0063] Eudragit S100 300g

[0064] Triethyl citrate 60g

[0065] Talc powder 6g

[0066] Titanium dioxide 30g

[0067] Iron Oxide Red 30g

[0068] Ethanol 4750ml

[0069] water 250ml

[0070] Coating process: Prepare the above coating solution according to the con...

Embodiment 3

[0072] Tablet prescription:

[0073] Mesalamine 1200g

[0074] Carbomer 971 25g

[0075] Dextran-40 75g

[0076] Magnesium Stearate 13.0g

[0077]

[0078] 1000 pieces

[0079] The preparation process of the tablet core: mesalazine, carbomer 971, dextran-40, adding an appropriate amount of distilled water, granulating, and drying. Add magnesium stearate, mix uniformly, measure the granule content, compress into tablets, and the main ingredient content of each tablet is 1.2g.

[0080] Coating Solution Prescription:

[0081] Coating Material Weight

[0082] Eudragit S100 200g

[0083] Eudragit L100 150g

[0084] Triethyl citrate 60g

[0085] Talc powder 6g

[0086] Titanium dioxide 30g

[0087] Iron Oxide Red 30g

[0088] Ethanol 4750ml

[0089] water 250ml

[0090] Coating process: Prepare the above coating solution according to the conventional method, and coat with a high-efficienc...

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PUM

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Abstract

The invention relates to a mesalazine oral colon-targeted sustained release medicine composition which is characterized by containing: (a) a sustained release table core containing mesalazine or medicinal salts or solvates thereof and hydrophilic stroma, wherein the mesalazine or the medicine salts thereof are dispersed in the hydrophilic stroma; and (b) a coating wrapped outside the table core and containing acid-resistant materials; wherein the one-hour release of the composition in simulated intestinal fluid with the pH of 7.2 is less than 20 percent, the four-hour release thereof is 30-60 percent, and the eight-hour release thereof is greater than 70 percent. The composition has simple manufacturing process and low cost, slowly releases the mesalazine in small intestines and colons, and achieves the colon-targeted medicine delivery once a day and the local curative effect.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a colon-targeted slow-release pharmaceutical composition for oral administration of mesalazine, a controlled-release tablet core containing mesalazine or its pharmaceutically acceptable salt or its solvate and a hydrophilic matrix, and the tablet core is coated with One layer of coating contains an acid-resistant material, and the composition releases less than 20% in 1 hour, 30-60% in 4 hours, and more than 70% in 8 hours in simulated intestinal fluid with pH 7.2. The composition gradually releases mesalamine in the small intestine and colon, and is used for treating colitis with intestinal targeted administration once a day. Background technique [0002] Inflammatory bowel disease is a general term for ulcerative conjunctivitis and Crohn's disease, which together affect 0.5-1.0% of the western population, with more than 1 million patients in the United States and more...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K31/606A61P1/04
Inventor 王显著王海屿邓杰张涛牟才华
Owner CHONGQING PHARMA RES INST
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