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Erdosteine ​​compound for treating respiratory inflammation and preparation method thereof

A technology for erdosteine ​​and a compound, which is applied to the erdosteine ​​compound for treating respiratory tract inflammation and the field of preparation thereof, can solve the problems of drug absorption speed or degree, poor water solubility of erdosteine, low effective bioavailability, etc. problem, to achieve the effect of high stability, convenient preparation, and improved water solubility

Inactive Publication Date: 2016-08-24
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 dissolves very slowly, there may be problems with the rate or extent of drug absorption in the formulation
[0006] Existing approaches to solve the poor water solubility of erdosteine ​​mainly include changing the dosage form, such as CN101606931B making it into dispersible tablets. Although the above preparations have improved the water solubility of the drug to a certain extent, there are also many defects.

Method used

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  • Erdosteine ​​compound for treating respiratory inflammation and preparation method thereof
  • Erdosteine ​​compound for treating respiratory inflammation and preparation method thereof
  • Erdosteine ​​compound for treating respiratory inflammation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 ： Preparation of erdosteine ​​compound

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

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

[0034] (3) After adding the solution, let it stand for 2 hours, add -15°C sodium chloride saturated solution dropwise under the condition of stirring at 80 rpm, the volume of the saturated sodium chloride solution is 5 times the weight of erdosteine, The uniform dropwise addition is completed within 0.5h;

[0035] (4) After the dropwise addition, the temperature was lowered to -15°C, and the stirring was continued at a...

Embodiment 2

[0037] Example 2 ： Preparation of erdosteine ​​compound

[0038] (1) Grind the crude erdosteine, pass 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, 100 rpm stirring for 20 minutes;

[0039] (2) Under stirring at 495 rpm, add a tetrahydrofuran:water mixed solution with a volume ratio of 1:3.5 whose volume is 10 times the weight of erdosteine, and raise the temperature to 33°C at the same time;

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

[0041] (4) After the dropwise addition, the temperature was lowered to -5°C, and the stirring ...

Embodiment 3

[0043] Example 3 ：Preparation of erdosteine ​​compound

[0044] (1) Grind the crude erdosteine, pass through a 200-mesh sieve, and then add it to a mixed solution of isopropanol and propyl formate whose volume is 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) Under stirring at 560 rpm, add a mixed solution of tetrahydrofuran with a volume 12 times the weight of erdosteine: water with a volume ratio of 1:3.5, and raise the temperature to 45°C at the same time;

[0046] (3) After adding the solution, let it stand for 3 hours, and add a saturated solution of sodium chloride at 5°C dropwise under the condition of stirring at 120 rpm. The volume of the saturated solution of sodium chloride is 8 times the weight of erdosteine, 0.5 The uniform dropwise addition is completed within h;

[0047] (4) After the dropwise addition, the temperature was lowered to 5°C, and the stirring w...

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PUM

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Abstract

The invention discloses an erdosteine ​​compound for treating respiratory inflammation and a preparation method thereof, belonging to the technical field of medicine. The X-ray powder diffraction pattern obtained by measuring the erdosteine ​​compound using Cu-Kα rays is shown in Figure 1. The erdosteine ​​crystal provided by the invention has stable chemical properties, good water solubility and high stability, brings convenience to the preparation of 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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Patent Type & Authority Patents(China)
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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