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Mesalazine gel and preparation method thereof

A technology of mesalazine and gel, which is applied in the field of mesalazine gel and its preparation, can solve the problems of unsatisfactory rectal curative effect, irritation of gastrointestinal tract, liver damage, etc., and improve bioavailability and patient compliance, easy to clean, and long-lasting effects

Pending Publication Date: 2021-04-02
重庆健能医药开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The existing medicines for the treatment of colitis in China are mainly taken orally. Oral medicines are irritating to the gastrointestinal tract and damage the liver, and the curative effect of oral medicines on the rectum is not ideal.

Method used

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  • Mesalazine gel and preparation method thereof
  • Mesalazine gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: the preparation of test sample

[0026] Prepare 1200g of gel containing mesalazine, the amount of raw materials and auxiliary materials is: 80g of mesalazine, 8g of carbomer, 1g of sodium benzoate, 4g of potassium metabisulfite, 60g of glycerin, 6g of triethanolamine, appropriate amount of potassium acetate, The rest is distilled water.

[0027] The steps of the preparation method are as follows: 1. Treat the main drug so that its particle size is controlled at 30um, and take the processed main drug according to the formula for future use. 2. Dissolving preservatives: take sodium benzoate according to the formula, add appropriate amount of degassed purified water and stir to dissolve. 3. Preparation of matrix: Grind the formulated amount of carbomer with the formulated amount of glycerin or propylene glycol for use, and add the treated carbomer into the 2 solution under stirring to make it fully swell. Then add potassium metabisulfite, triethanolamine an...

Embodiment 2

[0033] Embodiment 2 Action investigation

[0034] (1) Dissolution test:

[0035] Experimental method: According to the fourth method of the four general rules of the Chinese Pharmacopoeia in 2015, the in vitro dissolution rate of mesalazine gel and enema was determined. Ultrasonic degassed PBS (pH6.8) was used as the release medium at a temperature of 37±0.5°C. At a speed of 50r / min, take 5ml of the release solution for 5min, 10min, 15min, 20min, 30min, 45min, and 60min and supplement it with an equal amount of blank release medium at the same temperature. After filtering through a microporous membrane, take the subsequent filtrate for ultraviolet measurement.

[0036] Result: if figure 1 shown by figure 1 It can be seen that the dissolution rate of the gel of mesalazine is faster than that of the imported enema.

[0037] (2) In vivo pharmacokinetic experiments:

[0038] experimental method:

[0039] 20 SD rats, weighing 250±20g, were fasted for 1 day before the test, ...

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Abstract

The invention discloses gel containing mesalazine. The gel is prepared from the following raw material medicines and auxiliary materials in parts by weight: 30-120 parts of mesalazine, 7-15 parts of matrix, 0.5-2 parts of sodium benzoate, 2-10 parts of antioxidant, 40-110 parts of glycerol or propylene glycol and 5-10 parts of triethanolamine; a proper amount of potassium acetate is added to regulate pH to 4-5 and 1200 parts of distilled water are added. The mesalazine gel is made of a polymer gel-forming material, so that the appearance is uniform, and the physical stability is good; the mesalazine gel has good affinity with the intestinal mucosa, and has high penetrability, so that the curative effect is enhanced; and the gel is convenient to use, and stays in the intestinal tract for alonger time in comparison with an enema, thereby extending the drug action time.

Description

technical field [0001] The invention relates to a gel for treating ulcerative colitis by rectal administration and a preparation method thereof. Background technique [0002] Chronic colitis (ulcerativecolitis) is a worldwide distribution disease, its incidence rate is 5-12 / 100,000 in the west, prevalence rate is 50-150 / 100,000; to an upward trend. [0003] Mesalazine was developed by Sanofi, and later authorized to Meda in the United States, and Kyorin Pharmaceutical in Japan, with various formulations on the market. [0004] Mesalazine is affected by the hepatic first-pass effect and has low bioavailability. However, conventional clinical oral dosage forms such as capsules and tablets all have the problems of frequent administration and poor patient compliance. Therefore, there is an urgent need to develop a new dosage form of mesalazine. [0005] Domestic existing medicines for the treatment of colitis are mainly oral. Oral medicines are irritating to the gastrointesti...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K47/10A61K47/12A61K31/606A61P1/00A61P1/04
CPCA61K9/06A61K31/606A61K47/10A61K47/12A61P1/00A61P1/04
Inventor 韦维叶世春朱姣
Owner 重庆健能医药开发有限公司
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