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Sodium acetylcysteine for removing phlegm and curing hepatopathy and preparation method thereof

A technology of sodium cysteine ​​and acetyl, which is applied in the field of sodium acetylcysteine ​​and its preparation, can solve problems such as instability and difficulty in synthesis, and achieve good stability, good medicinal effect, and high purity

Inactive Publication Date: 2007-10-17
邵长青
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

From the structural point of view, acetylcysteine ​​contains sulfhydryl groups, which is very unstable. If certain measures are not taken, it is difficult to synthesize a relatively pure medicinal product-sodium acetylcysteine ​​in the aqueous or organic phase.

Method used

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  • Sodium acetylcysteine for removing phlegm and curing hepatopathy and preparation method thereof
  • Sodium acetylcysteine for removing phlegm and curing hepatopathy and preparation method thereof
  • Sodium acetylcysteine for removing phlegm and curing hepatopathy and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0101] Embodiment 1: preparation sodium acetylcysteine

[0102] 1. Weigh 50g (0.306mol) of acetylcysteine, put it in a three-necked flask, add 136ml of analytically pure methanol, put it in a water bath at 15°C, add 0.5g of sulfhydryl protecting agent DTT (dithiothreitol), and stir for 30 minutes. Add water-removing agent molecular sieve 15g.

[0103] 2. Weigh 14.2g of NaOH and add it into the methanol solution in 6 times with an interval of 1h between each time.

[0104] 3. After adding NaOH for the sixth time, continue to react in a water bath at 15° C. with stirring for 1 h. Then, the reaction flask was moved into a water bath at 20-25°C and stirred for 1 h. Suction filtration, filter out the molecular sieves, add the filtrate to 400ml acetone, shake well to make the mixture even.

[0105] 4. After a large amount of white precipitates appeared in the reaction solution, filter with suction, and dry the filter cake at 80° C. to obtain 40.5 g of sodium acetylcysteine, with ...

Embodiment 2

[0107] Embodiment 2: preparation sodium acetylcysteine

[0108] Weigh 50 g (0.306 mol) of acetylcysteine, put it in a three-necked flask, add 136 ml of analytically pure methanol, put it in a water bath at 15°C, add 0.5 g of thiol protecting agent 2-mercaptoethanol and 10 g of molecular sieves, and stir for 15 min. The preparation method is the same as in Example 1 except that the thiol protecting agent added is different.

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Abstract

The present invention relates to a sodium acetylcysteine medicine for curing acute and chronic hepatopathy, which have above structural formula. The present invention also provides method for preparation of above sodium acetylcysteine, including performing acid-base salt reaction in general organic solvent by using acetylcysteine reacting with general inorganic base, which assisted by mercapto protecting agent and reaction system de-watering agent during the reaction process, adding precipitating agent to precipitate after reaction is finished, then preparing sodium acetylcysteine by filtrating and drying. The sodium acetylcysteine provided in present invention has advantages of high stability, low toxicity, exact curative effect and convenience in clinic application.

Description

technical field [0001] The invention relates to the field of medicines and preparation methods thereof, in particular, the invention relates to sodium acetylcysteine ​​and a preparation method thereof. Sodium acetylcysteine ​​is mainly used for expectorant and treatment of acute and chronic liver diseases. Background technique [0002] Acetylcysteine ​​(English name: Acetylcysteine, chemical name: acetylcysteine) has a variety of medicinal uses: 1. As an expectorant for mucus dissolving agent, 2. Acetylcysteine ​​for injection As a hepatoprotective drug, it is used to treat acute and chronic liver diseases and drug-induced liver injury. Its molecular formula: C 5 h 9 N0 3 S, molecular weight: 163.20, structural formula as follows: [0003] [0004] Oral preparations, lyophilized powder injections and aqueous injections of the product are currently on the market. Due to the strong acidity of this product, most of the existing preparations are formulated as neutral fo...

Claims

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Application Information

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IPC IPC(8): C07C323/59C07C319/12A61K31/198A61P11/10A61P1/16
Inventor 邵长青
Owner 邵长青
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