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New medical application of ritonavir to enhancing anti-inflammation effect of glucocorticoid

A glucocorticoid and ritonavir technology, applied in the field of chemical medicine, can solve problems such as slowing down the spread of HIV

Inactive Publication Date: 2016-12-07
BINZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Clinical anti-HIV protease inhibitor (protease inhibitor) ritonavir (indicated for the treatment of adult HIV-I infection, for human immunodeficiency virus-1 (HIV-1) and human immunodeficiency virus-2 (HIV-2) aspartic acid Orally effective inhibitor of protease, blocking the enzyme to promote the polyprotein required to produce morphologically mature HIV particles, so that HIV particles remain in an immature state, thereby slowing down the spread of HIV in cells to prevent new The occurrence of round infection and delay the development of the disease, but the pharmacological effects of anti-HIV protease inhibitors combined with glucocorticoids to prevent or treat tolerance caused by long-term use of glucocorticoids have not been reported

Method used

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Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0012] Experimental example 1 Effect of anti-HIV protease inhibitor ritonavir on GRα and phosphorylated NF-κB in pulmonary microvascular endothelial cells stimulated by LPS

[0013] 1.1 Drugs and reagents

[0014] The DMEM medium is the product of Gibco Company, and the newborn bovine serum is the product of Hangzhou Sijiqing Company

[0015] LPS (product of Sigma, purchased from Dalian Meilun Biotechnology Co., Ltd.)

[0016] Ritonavir (purity 99.3%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0017] GRα antibody (Glucocorticoid Receptor (D8H2) Rabbit mAb, cellsignal company, Cat. No.: 3660s) Human pulmonary microvascular endothelial cells (Cell Bank of Chinese Academy of Sciences)

[0018] Methylprednisolone (methylprednisolone sodium succinate for injection, produced by Pfizer, 500mg / bottle)

[0019] 1.2 Experimental methods and results

[0020] When the pulmonary microvascular endothelial cells grew and merged to 70%-80%, fresh culture medium was chan...

experiment example 2

[0024] Experimental Example 2 Effect of Anti-HIV Protease Inhibitor Ritonavir on LPS-induced Acute Respiratory Distress Syndrome (ALI / ARDS) Model Rats

[0025] 2.1 Drugs and reagents

[0026] LPS (product of Sigma, purchased from Dalian Meilun Biotechnology Co., Ltd.)

[0027] Ritonavir (purity 99.5%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0028] Methylprednisolone (methylprednisolone sodium succinate for injection, produced by Pfizer, 500mg / bottle)

[0029] GRα antibody (Glucocorticoid Receptor (D8H2) Rabbit mAb, cellsignal company, catalog number: 3660s)

[0030] 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.

[0031] 2.2 Experimental methods and results

[0032] 2.2.1 Preparation, grouping and administration of endotoxin double-hit ARDS rat model

[0033]70 male r...

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PUM

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Abstract

The invention provides new medical application of ritonavir, and particularly relates to the medical application of ritonavir and glucocorticoid in cooperation to enhancing the anti-inflammation effect of glucocorticoid. In the application, the range of oral dosage is 100-2400 mg, preferentially 100-1200 mg.

Description

technical field [0001] The invention belongs to the field of chemical medicine, and specifically relates to the combined use of anti-HIV protease inhibitor ritonavir and glucocorticoids, enhancing the anti-inflammatory effect of glucocorticoids and treating the tolerance caused by long-term use of glucocorticoids in the treatment of acute respiratory distress syndrome . Background technique [0002] Glucocorticoid (GC) is a class of steroid hormones secreted by the adrenal cortex. Glucocorticoids have rapid, potent and nonspecific anti-inflammatory effects. Effective for all kinds of inflammation. In the early stage of inflammation, GC inhibits telangiectasia, relieves exudation and edema, and inhibits infiltration and phagocytosis of white blood cells, thereby reducing inflammatory symptoms. In the late stage of inflammation, it inhibits the proliferation of capillaries and fibroblasts, and delays the formation of granulation tissue. And reduce the sequelae of inflammat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/427A61K31/573A61P11/00A61P29/00
CPCA61K31/427A61K31/573A61K2300/00
Inventor 蒋王林张广华纪云霞叶亮朱海波
Owner BINZHOU MEDICAL COLLEGE
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