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Special ultrafine tiopronin powder lyophilized preparation and preparation method thereof

An ultra-fine powder, tiopronin technology, applied in the field of medicine, can solve the problems of low clarity of tiopronin, small specific surface area, large toxic and side effects, etc. Effect

Inactive Publication Date: 2014-11-26
杭州长典老一元健康管理有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Existing tiopronin has the disadvantages of low clarity, poor stability, low purity, many impurities, large particles, small specific surface area, poor solubility, large toxic and side effects, and easy allergies

Method used

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  • Special ultrafine tiopronin powder lyophilized preparation and preparation method thereof
  • Special ultrafine tiopronin powder lyophilized preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Add 163 grams (1.5 mol) of 2-chloropropionic acid and 68.7 grams (0.5 mol) of phosphorus trichloride to a dry 500ml reaction bottle, stir and react under the condition of blocking moisture, and react for 4 hours at a reaction temperature of 40°C to generate 2 - Chloropropionyl chloride. After the reaction was finished, the distillate at 107-113° C. was collected by distillation to obtain 181 grams of 2-chloropropionyl chloride as a colorless liquid, with a yield of 95%. Add 37.5 g (0.5 mol) of glycine, 26.5 g (0.25 mol) of anhydrous sodium carbonate and 250 ml of water to a 1000 ml reaction bottle, stir to dissolve. Cool in an ice-salt bath, add 63.5 g (0.5 mol) of 2-chloropropionyl chloride dropwise under vigorous stirring, and control the reaction temperature at -5°C. At the same time, add a saturated solution of anhydrous sodium carbonate to make the reaction solution weakly alkaline. After the addition was complete, the stirring reaction was continued for 3 hours. ...

Embodiment 2

[0030]Add 163 grams (1.5 mol) of 2-chloropropionic acid and 68.7 grams (0.5 mol) of phosphorus trichloride to a dry 500ml reaction bottle, stir and react under the condition of blocking moisture, and react at a reaction temperature of 45°C for 3.5 hours to generate 2 - Chloropropionyl chloride. After the reaction, the distillate at 107-113° C. was collected by distillation to obtain 183 grams of 2-chloropropionyl chloride as a colorless liquid, with a yield of 96.1%. Add 37.5 g (0.5 mol) of glycine, 26.5 g (0.25 mol) of anhydrous sodium carbonate and 250 ml of water to a 1000 ml reaction bottle, stir to dissolve. Cool in an ice-salt bath, add 63.5 g (0.5 mol) of 2-chloropropionyl chloride dropwise under vigorous stirring, and control the reaction temperature at -10°C. At the same time, add a saturated solution of anhydrous sodium carbonate to make the reaction solution weakly alkaline. After the addition was complete, the stirring reaction was continued for 4 hours. After th...

Embodiment 3

[0038] Add 163 grams (1.5 mol) of 2-chloropropionic acid and 68.7 grams (0.5 mol) of phosphorus trichloride to a dry 500ml reaction bottle, stir and react under the condition of blocking moisture, and react at a reaction temperature of 50°C for 3 hours to generate 2 - Chloropropionyl chloride. After the reaction, the distillate at 107-113° C. was collected by distillation to obtain 182 grams of 2-chloropropionyl chloride as a colorless liquid, with a yield of 95.6%. Add 37.5 g (0.5 mol) of glycine, 26.5 g (0.25 mol) of anhydrous sodium carbonate and 250 ml of water to a 1000 ml reaction bottle, stir to dissolve. Cool in an ice-salt bath, add 63.5 g (0.5 mol) of 2-chloropropionyl chloride dropwise under vigorous stirring, and control the reaction temperature at -15°C. At the same time, add a saturated solution of anhydrous sodium carbonate to make the reaction solution weakly alkaline. After the addition was complete, the stirring reaction was continued for 5 hours. After the...

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Abstract

The invention discloses a special ultrafine tiopronin powder lyophilized preparation and a preparation method thereof. The preparation method comprises the following steps: reacting 2-chloropropionic acid with phosphorus trichloride to generate 2-chloropropionyl chloride, reacting 2-chloropropionyl chloride with glycine to generate 2-chloropropionyl glycine, reacting 2-chloropropionyl glycine with sodium disulfide, reducing by zinc powder to obtain crude tiopronin, purifying, carrying out air jet ultrafine crushing, and lyophilizing to prepare the special ultrafine tiopronin powder lyophilized preparation. The special ultrafine tiopronin powder lyophilized preparation has the advantages of good clarity, high stability, high purity, few impurities, small particle size, large specific surface area, good solubility, small toxic side effects, difficult allergy and the like.

Description

technical field [0001] The invention relates to a special ultrafine powder freeze-dried preparation of tiopronin and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Tiopronin, Chinese chemical name: N-(2-Mercaptopropionyl)-glycine, English chemical name: N-(2-Mercaptopropionyl)glycine. Tiopronin is a new type of glycine derivative containing free sulfhydryl groups. Tiopronin has a detoxification effect, protects liver tissue and cells, has a significant repair effect on alcohol-induced liver damage, and improves liver function. Tiopronin is a thiol-containing drug similar in nature to penicillamine, and has the effect of protecting liver tissue and cells. Animal experiments have shown that tiopronin can prevent liver damage caused by carbon tetrachloride, ethionine, acetaminophen, etc. by providing sulfhydryl groups, and can inhibit the accumulation of triglycerides in chronic liver damage. Tiopronin can reduce the...

Claims

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Application Information

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IPC IPC(8): C07C323/60C07C319/02A61K9/19A61K31/198
Inventor 傅苗青李凤生陈宇东
Owner 杭州长典老一元健康管理有限公司
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