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Crystalline pharmaceutical compound and preparation method and usage thereof

A pharmaceutical compound and crystallization technology, which is applied in the field of S--cysteine ​​pharmaceutical compound and its preparation, can solve problems such as damage to gastrointestinal mucosa, irritation of the digestive tract, bleeding, ulcers and even perforation, and achieve water content differences Small, stable, not easy to absorb moisture

Active Publication Date: 2014-04-16
GUANGZHOU BAIYUNSHAN PHARMA HLDG CO LTD BAIYUNSHAN PHARMA GENERAL FACTORY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] As an expectorant drug, carbocisteine ​​is widely produced and used in my country, but there are two carboxyl groups in the structure of carbocisteine, which is acidic, which makes the drug irritating to the digestive tract and can cause gastric Adverse reactions such as discomfort, nausea, vomiting, gastrointestinal bleeding
If the drug is taken for a long time, it is easy to damage the gastrointestinal mucosa, leading to serious side effects such as bleeding, ulcers and even perforation.

Method used

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  • Crystalline pharmaceutical compound and preparation method and usage thereof
  • Crystalline pharmaceutical compound and preparation method and usage thereof
  • Crystalline pharmaceutical compound and preparation method and usage thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0108] At room temperature, in a three-necked flask equipped with a stirring device, add 50g of S-(carboxymethyl)-L-cysteine, 40ml of distilled water, and then add 25ml of 25% ammonia water to the obtained suspension, and stir quickly to obtain clarification solution, drop 600ml of ethanol therein, at the beginning the dropping speed is slightly faster, and when white crystals are precipitated, the dropping speed is slowed down; , and dried to obtain 56.5 g of white S-(carboxymethyl)-L-cysteine ​​ammonium salt monohydrate crystals, with a yield of about 94.5%.

Embodiment 2

[0110] At room temperature, in a three-neck flask equipped with a stirring device, add 25g of S-(carboxymethyl)-L-cysteine, 20ml of distilled water, and then add 14ml of 25% ammonia water to the obtained suspension, and stir quickly to obtain clarification Solution, add 400ml of isopropanol dropwise therein, the drop rate is slightly faster at the beginning, and slow down the drop rate when white crystals are precipitated. The filter cake was washed, drained, and dried to obtain 28.5 g of white S-(carboxymethyl)-L-cysteine ​​ammonium salt monohydrate crystals, with a yield of about 95.4%.

Embodiment 3

[0112] At room temperature, in a three-neck flask equipped with a stirring device, add 50g of S-(carboxymethyl)-L-cysteine, 40ml of distilled water, and then add 30ml of 25% ammonia water to the obtained suspension, and stir quickly to obtain clarification solution, drop 600ml of acetone therein, at the beginning the dropping speed is slightly faster, and when white crystals are precipitated, the dropping speed is slowed down; , and dried to obtain 57.4 g of white S-(carboxymethyl)-L-cysteine ​​ammonium salt monohydrate crystals, with a yield of about 96.0%.

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Abstract

The invention relates to an S-(carboxymethyl)-L-cysteine ammonium salt water crystalline pharmaceutical compound (having the following structural formula) and a preparation method and the application of the compound in the preparation of medicines for eliminating phlegm as well as medicines for preventing and treating respiratory system diseases such as chronic obstructive pulmonary diseases (COPD) and the like. After the compound is adopted, the COPD model rat airway resistance is remarkably reduced, the generation of oxide is reduced, the antioxidant level is increased, and the damage of oxide, inflammatory mediator and the like to the lung can be relieved.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, in particular, the invention relates to an S-(carboxymethyl)-cysteine ​​pharmaceutical compound and its preparation method and application. Background technique [0002] Carbocisteine, whose chemical name is S-(carboxymethyl)-L-cysteine ​​(carbocisteine, carboxymethylcysteine, CMC), was first developed and applied clinically by the French Joullie company in 1961. It is a mucolytic drug, It can affect the secretion of bronchial glands, increase the secretion of low-viscosity salivary mucin, reduce the production of high-viscosity fucoidal mucin, and directly act on the disulfide bond of mucin to crack mucin molecules and reduce sputum. Viscous fluid, easy to spit out; can improve mucociliary clearance rate; reduce airway hyperresponsiveness. After CMC enters the body, it is easy to remove the carboxymethyl group to form cysteine, and the sulfhydryl group contained in it can interact with electrop...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C323/58C07C319/14A61K31/198A61P11/10A61P11/00
Inventor 钟南山陈矛朱少璇郑劲平万平王玮莫红缨廖维胡海容余瑜傅祥麟冯金黄冰娥张琳
Owner GUANGZHOU BAIYUNSHAN PHARMA HLDG CO LTD BAIYUNSHAN PHARMA GENERAL FACTORY
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