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Application of Saquigravir in the preparation of drugs for preventing or treating pulmonary fibrosis

A technology for pulmonary fibrosis and drugs, applied in the application field of saquigravir in the preparation of drugs for the prevention or treatment of pulmonary fibrosis, can solve the problem of reducing the total amount of HIV in the blood, pharmacological effects have not been reported, loss of binding and hydrolysis Fragmented peptides, etc.

Inactive Publication Date: 2016-05-18
BINZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Clinically, Saquinavirmesylate (Invirase) is a highly efficient and highly selective HIV protease inhibitor, which acts on the late stage of HIV reproduction and binds to the activation point of HIV protease, causing it to lose its binding and hydrolyze the broken polypeptide. Function, combined with other drugs to treat severe HIV infection, increase CD4 count, 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 Saquigravir in the preparation of drugs for preventing or treating pulmonary fibrosis
  • Application of Saquigravir in the preparation of drugs for preventing or treating pulmonary fibrosis
  • Application of Saquigravir in the preparation of drugs for preventing or treating pulmonary fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1 Preparation of Saquilavir Mesylate Lyophilized Powder Injection

[0013] Take 50.0g of saquilavir mesylate, add 2000ml of water for injection to dissolve it, add 8g of mannitol, stir to dissolve, ultrafiltration to obtain a pyrogenic clear liquid, pour it into a 10ml vial, 2ml / piece, and freeze The dry powder injection process is freeze-dried to make each freeze-dried powder injection containing 50.0 mg of saquilavir mesylate.

Embodiment 2

[0014] Example 2 Preparation of saquinavir mesylate capsules

[0015] Weigh 200.0g of saquilavir mesylate and 100.0g of sodium carboxymethyl starch, mix well, pass through a 100-mesh sieve, and add an appropriate amount of 3% PVP K30 Prepare soft material with appropriate amount of aqueous solution, granulate with 20 mesh sieve, dry at 60°C for 3 hours, sizing on 18 mesh sieve, add 2.0g magnesium stearate, mix well and then encapsulate, adjust the capsule weight to about 300mg, it is ready.

experiment example 2

[0027] Experimental Example 2 The effect of saquinavir 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] Saquilavir mesylate (purity 99.5%, purchased from Dalian Meilun Biological Technology Co., Ltd.)

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

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

[0032] RAGE primary antibody was purchased from sigma company.

[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 certificate number is: SYXK (鲁)20030020.

[0034] 2.2 Experimental methods and results

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

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

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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 saquilavir inhibiting the occurrence and development of acute lung injury / acute respiratory distress syndrome (ALI / ARDS) and pulmonary fibrosis, thereby preventing or treating ALI / ARDS and pulmonary fibrosis; in particular, it relates to the inhibition of I Type I alveolar epithelial cell apoptosis promotes the expression of receptor for advanced glycation end products (RAGE) of 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 very high mortality rate, which seriously threatens the lives of critically ill patients and affects their quality of life. ALI / ARDS is the acute hypoxic respiratory function caused by the damage of lung capillary endothelial cells and alveolar epithelial cells in the process of non-cardiogenic diseases such as severe infection, s...

Claims

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Application Information

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Patent Type & Authority Patents(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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