Application of darunavir ethanolate in preparing medicine for preventing or treating acute lung injury/acute respiratory distress syndrome and pulmonary fibrosis

A technology of darunavir ethanol salt and pulmonary fibrosis, applied in the field of application of darunavir ethanol salt in the preparation of drugs for the prevention or treatment of acute lung injury/acute respiratory distress syndrome and pulmonary fibrosis, can solve Pharmacological effects have not been reported and other issues

Inactive Publication Date: 2014-08-20
BINZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Darunavir ethalolate (also known as "Darunavir", trade name prezista) is suitable for the treatment of HIV infection in adults who are ineffective for other anti-HIV drugs when used in combination with small doses of ritonavir or other anti-HIV drugs. It is a new HIV-1 protease inhibitor. Its mechanism of action is to selectively inhibit the HIV cleavage of the coding Gag-Pol polyprotein in infected cells, and then inhibit the formation of mature virus particles. However, darunavir ethanol salt is effective in preventing Or the pharmacological effects of treating ALI / ARDS and pulmonary fibrosis have not been reported

Method used

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  • Application of darunavir ethanolate in preparing medicine for preventing or treating acute lung injury/acute respiratory distress syndrome and pulmonary fibrosis
  • Application of darunavir ethanolate in preparing medicine for preventing or treating acute lung injury/acute respiratory distress syndrome and pulmonary fibrosis
  • Application of darunavir ethanolate in preparing medicine for preventing or treating acute lung injury/acute respiratory distress syndrome and pulmonary fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1 Preparation of Darunavir Ethanol Salt Freeze-Dried Powder for Injection

[0013] Take 60.0g of darunavir ethanol salt, add 2000ml of water for injection to dissolve it, add 8g of mannitol, stir to dissolve, ultra-filter to obtain a clear solution without pyrogen, pour it into a 10ml vial, 2ml / bottle, press lyophilization The powder injection process was lyophilized to make each lyophilized powder injection containing 60.0 mg of darunavir ethanol salt.

Embodiment 2

[0014] Example 2 Preparation of Darunavir Ethanol Salt Film-Coated Tablets

[0015] Weigh 200.0g of darunavir ethanol salt and 100.0g of carboxymethyl starch sodium, mix well and pass through a 100-mesh sieve, add an appropriate amount of 3% PVP K30 Appropriate amount of water solution to prepare soft material, granulate with 20-mesh sieve, dry at 60°C for 3 hours, granulate with 18-mesh sieve, add 2.0g of magnesium stearate, mix well and then press into tablets. To prepare the coating solution, add pure water to the stainless steel container, then add the materials, keep stirring, and defoam. Coating Put the pressed tablet into the coating pan, spray coating after preheating, and continue the coating pan until the tablet is dry after spraying. Cool the dried sheet, add carnauba wax for polishing, and the sheet weighs about 300mg.

experiment example 2

[0027] Experimental example 2 Effect of darunavir ethanol salt on acute lung injury / acute respiratory distress syndrome (ALI / ARDS) model rats caused by cecal ligation and perforation

[0028] 2.1 Drugs and reagents

[0029] Darunavir ethanolate (purity 99.5%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0030] Limulus reagent kit (Fuzhou Xinbei Biochemical Industry Co., Ltd., Fujian Province, batch number: 080430)

[0031] Anti-Aquaporin5 antibody (abcam company, ab104751)

[0032] RAGE primary antibody was purchased from Sigma.

[0033] Experimental animals: SPF grade Sprague Dawley rats, male, weighing 150g-200g, provided by the Experimental Animal Center of Shandong Luye Pharmaceutical Co., Ltd., the animal qualification certificate number is: SYXK (Lu) 20030020.

[0034] 2.2 Experimental methods and results

[0035] 2.2.1 Preparation of rats with cecal ligation and puncture (CLP)

[0036] On the day of the operation, the rats were fasted in the morning,...

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Abstract

The invention provides novel use of a medicine darunavir ethanolate and particularly relates to an application of darunavir ethanolate for preventing or treating genesis and development of acute lung injury/acute respiratory distress syndrome (ALI/ARDS) and pulmonary fibrosis so as to prevent or treat ALI/ARDS and pulmonary fibrosis by inhibiting I type alveolar epithelial cells of alveolar epithelial cells and promoting expression of receptor for advanced glycation end products (RAGE) of the I type alveolar epithelial cells. According to the application, the injection dosage range is 120-2400mg, preferably 240-1200mg. The oral dosage range is 120-600mg, preferably 240-3000mg.

Description

technical field [0001] The present invention relates to darunavir ethanol salt to inhibit the occurrence and development of acute lung injury / acute respiratory distress syndrome (ALI / ARDS) and pulmonary fibrosis so as to prevent or treat ALI / ARDS and pulmonary fibrosis; specifically darunavir ethanol Salt can prevent or treat ALI / ARDS and pulmonary fibrosis by inhibiting the apoptosis of type I alveolar epithelial cells and promoting the expression of receptor for advanced glycation endproducts (RAGE) of type I alveolar epithelial cells. Background technique [0002] Acute lung injury / acute respiratory distress syndrome (ALI / ARDS) is a common critical illness with a high mortality rate, which seriously threatens the life of critically ill patients and affects their quality of life. ALI / ARDS is acute hypoxic respiratory function caused by diffuse pulmonary interstitial and alveolar edema caused by damage to pulmonary capillary endothelial cells and alveolar epithelial cells d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/635A61P11/00
Inventor 蒋王林纪云霞亢泽春徐洋
Owner BINZHOU MEDICAL COLLEGE
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