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Application of rivaroxaban in pharmaceuticals and pharmaceutical preparation

A technology of rivaroxaban and pharmaceutical preparations, applied in the field of rivaroxaban in pharmaceuticals and pharmaceutical preparations, can solve the problems of high fatality rate, achieve the effects of saving resources, shortening the research and development cycle, and reducing research costs

Inactive Publication Date: 2018-06-22
WUHAN POLYTECHNIC UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the incidence of AHS is only 0.1%, the fatality rate is as high as 20%.

Method used

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  • Application of rivaroxaban in pharmaceuticals and pharmaceutical preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Verification of the effect of rivaroxaban on inhibiting xanthine oxidase activity

[0031] Xanthine Oxidase (XO, EC 1.17.3.2) is a highly specific enzyme that can not only catalyze hypoxanthine to xanthine, and then uric acid, but also directly catalyze xanthine to uric acid. The present invention proves that rivaroxaban can inhibit the activity of xanthine oxidase to prevent and / or treat hyperuricemia.

[0032] Allopurinol is a urate-lowering drug widely used at present. It is a competitive xanthine oxidase inhibitor, which produces urate-lowering effect by inhibiting uric acid synthesis. The adverse reactions of allopurinol mainly include gastrointestinal symptoms, rash, liver function damage, bone marrow suppression, etc., about 5% of patients can not tolerate, and occasionally severe allopurinol hypersensitivity syndrome (allopurinol hypersensitivity syndrome, AHS ). The risk is increased in patients with renal insufficiency and with thiazide diuretics. ...

Embodiment 2

[0068] Example 2 Verification of the effect of rivaroxaban on lowering uric acid activity

[0069] Allopurinol is currently the most widely used urate-lowering drug, and it is a competitive xanthine oxidase inhibitor that produces urate-lowering effects by inhibiting uric acid synthesis. The adverse reactions of allopurinol mainly include gastrointestinal symptoms, rash, liver function damage, bone marrow suppression, etc., about 5% of patients can not tolerate, and occasionally severe allopurinol hypersensitivity syndrome (allopurinol hypersensitivity syndrome, AHS ). The risk is increased in patients with renal insufficiency and with thiazide diuretics. Studies by Khanna et al. have confirmed that AHS is closely related to positive leukocyte antigen HLA-B5801 gene. The HLA-B58 positive rate of Chinese Han people is 6%-8%, while that of white people is only 2%. Although the incidence of AHS is only 0.1%, the case fatality rate is as high as 20%. In this example, allopurin...

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Abstract

The invention discloses application of rivaroxaban in pharmaceuticals and a pharmaceutical preparation and aims at providing drugs for preventing and / or treating the hyperuricemia and gout caused by hyperuricemia. The drugs are low in cost and good in pharmaceutical effect.

Description

technical field [0001] The invention relates to the field of biotechnology, in particular to the application of rivaroxaban in pharmacy and pharmaceutical preparations. Background technique [0002] With the improvement of people's living standards and changes in eating habits, the incidence of hyperuricemia and gout in my country has been increasing year by year in recent years. Hyperuricemia is a disease in which blood uric acid exceeds the normal value due to purine metabolism disorder and / or uric acid excretion disorder. It refers to the level of blood uric acid on an empty stomach twice on different days under a normal purine diet: male > 420 μmol / L, Women >360μmol / L, no clinical symptoms. When the human body is in the condition of hyperuricemia for a long time, uric acid is precipitated in the joints, soft tissues, cartilage and kidneys in the form of sodium salt, causing human organ and tissue lesions, leading to gout, and causing serious complications, includi...

Claims

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Application Information

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IPC IPC(8): A61K31/5377A61P19/06
CPCA61K31/5377
Inventor 赵玲杨博薛稳来陈新刘梁
Owner WUHAN POLYTECHNIC UNIVERSITY