Erdosteine compound for treating respiratory tract inflammation and preparation method of erdosteine compound

A technology of erdosteine ​​and its compound, which is applied in the field of erdosteine ​​compound and its preparation for treating respiratory inflammation, and can solve the problems of drug absorption speed or degree, poor water solubility of erdosteine, and slow drug dissolution rate, etc. , to achieve high stability, convenient preparation, and improved water solubility

Inactive Publication Date: 2015-07-22
NANTONG QIWU AGRI PROD CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Erdosteine ​​has poor water solubility and low effective bioavailability in the human body, and the absorption rate of the drug in the body is often determined by the speed of dissolution. The drug in the solid preparation must be disintegrated and dissolved before being absorbed. Then the process of turning into a solution, if the drug is not easily released from the formulation or the drug dis

Method used

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  • Erdosteine compound for treating respiratory tract inflammation and preparation method of erdosteine compound
  • Erdosteine compound for treating respiratory tract inflammation and preparation method of erdosteine compound
  • Erdosteine compound for treating respiratory tract inflammation and preparation method of erdosteine compound

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0031] Example 1: Preparation of Erdosteine ​​Compound

[0032] (1) Grind the crude erdosteine, go through a 100-mesh sieve, and then add it to a mixed solution of isopropanol and propyl formate with a volume that is 3 times the weight of erdosteine. The volume of isopropanol and propyl formate The ratio is 1:4.5, stirring at 80 rpm for 15 minutes;

[0033] (2) Add a tetrahydrofuran:water volume ratio of 1:3.5 mixed solution with a volume of 8 times the weight of erdosteine ​​under stirring at 430 revolutions / min, and at the same time raise the temperature to 20°C;

[0034] (3) After the solution is added, let stand for 2 hours, and add -15℃ saturated sodium chloride solution dropwise under stirring at 80 rpm. The volume of the saturated sodium chloride solution is 5 times the weight of erdosteine. The dripping is completed at a constant speed within 0.5h;

[0035] (4) After the dropwise addition is completed, the temperature is lowered to -15°C, and the stirring is continued for 0....

Example Embodiment

[0037] Example 2: Preparation of Erdosteine ​​Compound

[0038] (1) Grind the crude erdosteine, go through a 150-mesh sieve, and then add it to a mixed solution of isopropanol and propyl formate whose volume is 4 times the weight of erdosteine. The volume of isopropanol and propyl formate The ratio is 1:4.5, stirring at 100 rpm for 20 minutes;

[0039] (2) Add a tetrahydrofuran:water volume ratio of 1:3.5 mixed solution with a volume of 10 times the weight of erdosteine ​​under stirring at 495 revolutions / min, while heating to 33°C;

[0040] (3) After the solution is added, let stand for 2.5 hours, and add -5°C saturated sodium chloride solution dropwise under stirring at 100 rpm. The volume of saturated sodium chloride solution is 6.5 times the weight of erdosteine. The dripping is completed at a constant speed within 0.5h;

[0041] (4) After the dropwise addition is completed, the temperature is lowered to -5°C, and the stirring is continued for 1.3 hours at a stirring rate of 12....

Example Embodiment

[0043] Example 3: Preparation of Erdosteine ​​Compound

[0044] (1) Grind the crude erdosteine, pass a 200-mesh sieve, and then add it to a mixed solution of isopropanol and propyl formate with a volume of 5 times the weight of erdosteine. The volume of isopropanol and propyl formate The ratio is 1:4.5, stirring at 120 rpm for 25 minutes;

[0045] (2) Add a mixed solution of tetrahydrofuran:water volume ratio 1:3.5 with a volume of 12 times the weight of erdosteine ​​under stirring at 560 revolutions / min, and at the same time heat to 45°C;

[0046] (3) After the solution is added, let stand for 3 hours, and add 5℃ saturated sodium chloride solution dropwise under stirring at 120 rpm. The volume of saturated sodium chloride solution is 8 times the weight of erdosteine, 0.5 The dripping is completed in h at a constant speed;

[0047] (4) After the dropwise addition is completed, the temperature is lowered to 5°C, and the stirring is continued for 2 hours at a stirring rate of 15 revol...

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Abstract

The invention discloses an erdosteine compound for treating respiratory tract inflammation and a preparation method of the erdosteine compound, belonging to the technical field of medicines. The X-ray powder diffraction patterns of the erdosteine compound measured by using Cu-K alpha rays are shown as the Figure 1. The erdosteine crystal provided by the invention is stable in chemical properties and high in water solubility, has high stability, brings convenience to various preparations and is very suitable for clinical application.

Description

technical field [0001] The invention relates to the field of medicine, and relates to an erdosteine ​​compound for treating respiratory inflammation and a preparation method thereof. Background technique [0002] Phlegm is the product of respiratory inflammation, which can irritate the respiratory mucosa, cause cough and asthma, and aggravate infection. When patients with acute and chronic bronchitis or chronic lung disease have respiratory failure, if the patient's sputum is too viscous or forms sputum plugs, it can block the airway and cause suffocation. Therefore, it is of great significance to use mucus sputum regulators to dissolve mucus sputum, make it thinner, lower its viscosity, accelerate the movement of mucous membranes and cilia in the respiratory tract, and improve the transport function. [0003] The currently marketed mucus regulators, such as bromhexine, sodium thioethanesulfonate, and carbocysteine, all have varying degrees of mucus regulation, but they hav...

Claims

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Application Information

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IPC IPC(8): C07D333/36A61K31/381A61P11/10A61P11/00A61P29/00
CPCC07B2200/13C07D333/36
Inventor 王玉美
Owner NANTONG QIWU AGRI PROD CO LTD
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