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Mesalazine oral sustained-release pharmaceutical composition and preparation method thereof

A technology for sustained-release medicines and compositions, which is applied in the directions of medicine combinations, pharmaceutical formulations, plant raw materials, etc., can solve the problems of increased alanine aminotransferase content, incomplete intestinal absorption, waste of mesalazine, etc., and achieves biocompatibility. The effect of improving sexuality, improving SOD activity and reducing MDA content

Inactive Publication Date: 2021-05-28
日照巴洛特药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The existing mesalamine oral sustained-release pharmaceutical composition, mesalamine will spread rapidly after taking it, so that the intestinal tract cannot be completely absorbed, and then a large amount of mesalamine is wasted, so that the patient has to take it many times a day, and the beauty Salazine can increase the level of alanine aminotransferase in the human body and cause liver damage

Method used

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  • Mesalazine oral sustained-release pharmaceutical composition and preparation method thereof
  • Mesalazine oral sustained-release pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] A mesalazine oral sustained-release pharmaceutical composition, comprising the following raw materials in parts by weight: 20 parts of mesalamine, 10 parts of red-backed leaf root extract, 10 parts of white peony extract, 50 parts of drug carrier, and 5 parts of xylitol , 3 parts of citric acid, 20 parts of carboxymethyl chitosan;

[0040] Described mesalamine oral sustained-release pharmaceutical composition is made by following steps:

[0041] Step S1: add mesalazine, red dorsal leaf root extract, white peony extract, and drug carrier into dichloroethane, stir for 5 minutes at a rotation speed of 300r / min, and a temperature of 30°C, and then add Lecithin continued to stir for 1h to obtain the first mixed solution;

[0042] Step S2: Add xylitol, citric acid, and deionized water into the reaction kettle, and stir until the xylitol and citric acid are completely dissolved to obtain a second mixed solution;

[0043] Step S3: Add carboxymethyl chitosan and deionized wate...

Embodiment 2

[0058] A mesalazine oral slow-release medicinal composition, comprising the following raw materials in parts by weight: 25 parts of mesalamine, 13 parts of red-backed leaf root extract, 13 parts of white peony extract, 55 parts of drug carrier, and 8 parts of xylitol , 5 parts of citric acid, 25 parts of carboxymethyl chitosan;

[0059] Described mesalamine oral sustained-release pharmaceutical composition is made by following steps:

[0060] Step S1: add mesalazine, red dorsal leaf root extract, white peony extract, and drug carrier into dichloroethane, stir for 10 minutes at a rotation speed of 400r / min, and a temperature of 35°C, and then add Lecithin continued to stir for 1.3h to obtain the first mixed solution;

[0061] Step S2: Add xylitol, citric acid, and deionized water into the reaction kettle, and stir until the xylitol and citric acid are completely dissolved to obtain a second mixed solution;

[0062] Step S3: Add carboxymethyl chitosan and deionized water into ...

Embodiment 3

[0077] A mesalamine oral sustained-release pharmaceutical composition, comprising the following raw materials in parts by weight: 30 parts of mesalamine, 15 parts of root extract of red dorsal leaves, 15 parts of white peony extract, 60 parts of drug carrier, and 10 parts of xylitol , 8 parts of citric acid, 30 parts of carboxymethyl chitosan;

[0078] Described mesalamine oral sustained-release pharmaceutical composition is made by following steps:

[0079] Step S1: add mesalazine, red dorsal leaf root extract, white peony extract, and drug carrier into dichloroethane, stir for 15 minutes under the conditions of rotation speed of 500r / min and temperature of 40°C, and then add Lecithin continued to stir for 1.5h to obtain the first mixed solution;

[0080] Step S2: Add xylitol, citric acid, and deionized water into the reaction kettle, and stir until the xylitol and citric acid are completely dissolved to obtain a second mixed solution;

[0081] Step S3: Add carboxymethyl ch...

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Abstract

The invention discloses a mesalazine oral sustained-release pharmaceutical composition and a preparation method thereof, and the mesalazine oral sustained-release pharmaceutical composition comprises the following raw materials by weight: 20-30 parts of mesalazine, 10-15 parts of a redback christmashush root extract, 10-15 parts of a white peony root extract, 50-60 parts of a drug carrier, 5-10 parts of xylitol, 3-8 parts of citric acid, and 20-30 parts of carboxymethyl chitosan. A drug carrier is prepared in the process of preparing the drug composition, the drug carrier takes cellulose acetate as a matrix and oxidizes the cellulose acetate, so that carboxyl is inserted into the surface of the cellulose acetate, and when the drug carrier is in contact with carboxymethyl chitosan, carboxyl on the drug carrier and primary amino of carboxymethyl chitosan form a polyelectrolyte membrane through positive and negative charge attraction, so that the biocompatibility of the drug carrier is improved, the medicine composition can be continuously released in intestinal tracts, the slow-release effect is achieved, absorption is prolonged, and the treatment effect of mesalazine is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an oral sustained-release pharmaceutical composition of mesalazine and a preparation method thereof. Background technique [0002] Mesalamine is the active ingredient of SASP for the treatment of ulcerative colitis, and it has a significant inhibitory effect on intestinal wall inflammation; mesalamine can inhibit the synthesis of prostaglandins that cause inflammation and the formation of inflammatory mediator leukotrienes, thereby affecting intestinal Mucosa inflammation plays a significant inhibitory role, mesalazine can inhibit the synthesis of prostaglandins in a dose-dependent manner, and reduce the release of PGE2 in human colonic mucosa. [0003] The existing mesalamine oral sustained-release pharmaceutical composition, mesalamine will spread rapidly after taking it, so that the intestinal tract cannot be completely absorbed, and then a larg...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/65A61K36/71A61K31/606A61K36/47A61K47/12A61K47/26A61K47/36A61K47/38A61P1/04A61K9/14
CPCA61K31/606A61K36/47A61K36/71A61K36/65A61K47/38A61K47/36A61K47/26A61K47/12A61K9/146A61K9/145A61P1/04A61K2236/333A61K2236/53A61K2236/51A61K2300/00
Inventor 刘加林方朝杰张渊源霍萧勇
Owner 日照巴洛特药业有限公司
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