Application of saquinavir mesilate in preparation of drug for preventing or treating acute lung injury/acute respiratory distress syndrome and pulmonary fibrosis

A technology for acute respiratory distress and acute lung injury, applied in the field of application of saquigravir in the preparation of drugs for the prevention or treatment of acute lung injury/acute respiratory distress syndrome and pulmonary fibrosis, can solve the problem of increasing CD4 count, pharmacological Unreported effects, loss of binding and hydrolysis of peptides and other issues

Inactive Publication Date: 2014-08-06
BINZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Clinically, Saquinavir mesylate (Invirase) is a high-efficiency and highly selective HIV protease inhibitor, which acts on the late stage of HIV reproduction, binds to the activation point of HIV protease, causes it to lose its binding and hydrolyzes the broken polypeptide It can be used in combination with other drugs to treat severe HIV infection, increase CD4 count, and reduce the total amount of HIV in the blood, but the pharmacological effects of saquigravir in the prevention or treatment of ALI / ARDS and pulmonary fibrosis have not been reported

Method used

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  • Application of saquinavir mesilate in preparation of drug for preventing or treating acute lung injury/acute respiratory distress syndrome and pulmonary fibrosis
  • Application of saquinavir mesilate in preparation of drug for preventing or treating acute lung injury/acute respiratory distress syndrome and pulmonary fibrosis
  • Application of saquinavir mesilate in preparation of drug 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 Saquigravir Mesylate Lyophilized Powder for Injection

[0013] Take 50.0g of saquigravir mesylate, add 2000ml of water for injection to dissolve it, add 8g of mannitol, stir to dissolve, and ultra-filter to obtain a pyrogen-free clear liquid, pour it into a 10ml vial, 2ml / bottle, and press to freeze The dry powder injection process was freeze-dried to make each freeze-dried powder injection containing 50.0 mg of saquigravir mesylate.

Embodiment 2

[0014] Example 2 Preparation of Saquigravir Mesylate Capsules

[0015] Weigh 200.0g saquigravir mesylate, and 100.0g 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 make soft material, granulate with 20-mesh sieve, dry at 60°C for 3 hours, sieve with 18-mesh sieve for granulation, add 2.0g of magnesium stearate, mix well and pack into capsules, adjust the weight of the capsules to about 300mg, and the product is ready.

experiment example 2

[0027] Experimental example 2 Effect of saquigravir mesylate 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] Saquigravir mesylate (purity 99.5%, purchased from Dalian Meilun 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, place...

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PUM

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Abstract

The invention provides new use of a drug of saquinavir mesilate and particularly relates to application of saquinavir mesilate for inhibiting occurrence and development of an acute lung injury / acute respiratory distress syndrome (ALI / ARDS) and pulmonary fibrosis by inhibiting I-type alveolar epithelial cell apoptosis to promote the expression of receptor for advanced glycation end products (RAGE), thus preventing or treating ALI / ARDS and pulmonary fibrosis. In the application, the range of the injection dosage is 50-2,000mg, preferably 50-1,000mg, and the oral dosage range is 200-6,000mg, preferably 400-6,000mg.

Description

technical field [0001] The present invention relates to saquigravir inhibiting 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 relate to saquigravir by inhibiting I Type I alveolar epithelial cell apoptosis, promote the expression of receptor for advanced glycation endproducts (RAGE) in type I alveolar epithelial cells, so as to prevent or treat ALI / ARDS and pulmonary fibrosis. 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 during non-cardiog...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/06A61P11/00
Inventor 蒋王林侯桂革纪云霞吕长俊
Owner BINZHOU MEDICAL COLLEGE
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