Application of orientin in preparation of drugs used for treating acute gout
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A technology for acute gout and drugs, applied in the application field of Orientin in the preparation of drugs for the treatment of acute gout, can solve problems such as neutropenia, aplastic anemia, etc., and achieve the effect of strong prevention and treatment activity and outstanding substantive characteristics
Inactive Publication Date: 2018-03-27
ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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Abstract
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Although they have fast anti-inflammatory and analgesic effects, their toxic and side effects are also quite obvious. For example, the effective dose of colchicine is similar to the dose that produces diarrhea and other gastrointestinal symptoms. Absolutely contraindicated in the case of bleeding, and the administration of phenylbutazone for as short as 3 weeks can also cause severe neutropenia or aplastic anemia
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Embodiment 1
[0020] Embodiment 1: the preparation of compound Orientin tablet involved in the present invention:
[0021] Take 5 grams of compound Orientin, add 195 grams of dextrin, mix well, and make 1000 tablets with a conventional tablet machine.
Embodiment 2
[0022] Embodiment 2: the preparation of the compound Orientin capsule involved in the present invention:
[0023] Take 5 grams of compound Orientin, add 195 grams of starch, mix well, and pack into capsules to make 1000 capsules.
[0024] The following pharmacodynamic experiments will further illustrate its drug activity.
experiment example 1
[0025] Experimental example 1: Orientin anti-acute gout inflammation experiment:
[0026] 1: method
[0027] ① Solution preparation
[0028] Add 5 g of uric acid and 1000 ml of distilled water to boil, add 5% NaOH solution to adjust the pH to 7.4, stir, cool and crystallize to make sodium urate crystals (MSU). The prepared MSU 10 mg was autoclaved, added 10 ml of serum-free DMEM culture solution, and ground to form a 1 mg / ml DMEM solution. During the experiment, this solution was added with DMEM culture medium to form MSU solutions with different concentrations of DMEM.
[0029] Orientin 2.5 mg, dissolved in dimethyl sulfoxide (DMSO), the final concentration of DMSO <0.02%, plus serum-free DMEM culture medium, prepared to a concentration of 2.5ug / ml, 25ug / ml, 250ug / ml.
[0030] Positive drug indomethacin 2.0mg, the method is the same as Orientin, the preparation concentration is 20ug / ml.
[0031] ② In vitro culture of vascular endothelial cells
[0032] Human umbilical ve...
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Abstract
The invention provides a new application of Orientin in medicine, specifically the application of Orientin in the preparation of medicine for treating acute gout. Experimental research results show that Orientin has a protective effect on the acute gout model of human vascular endothelial cell damage caused by urate, and inhibits the expression of ICAM‑1. Therefore, Orientin can be used to prepare a drug for treating acute gout inflammation. The use of Orientin involved in the present invention in the preparation of medicines for the treatment of acute gout is disclosed for the first time. Since the skeleton type belongs to a new skeleton type, and its preventive and treatment activity for acute gout is so strong that it is unexpected, there is no possibility of giving any inspiration from other compounds , has outstanding substantive features, and it is obviously a significant progress in the prevention and treatment of acute gout.
Description
technical field [0001] The present invention relates to a new application of compound Orientin, in particular to the application of Orientin in the preparation of medicines for treating acute gout. Background technique [0002] Gout, also known as gouty arthritis, is a disease caused by the disorder of purine metabolism in the body. It is manifested by excessive uric acid in the blood, and it is easy to cause urate (MSU) to crystallize in joints and other tissues. The acute attack of gout is due to the local neutrophil infiltration and inflammatory response caused by MSU deposited in the joints. [0003] Western medicine selects three kinds of medicines for use in the acute attack stage of gout: colchicine, non-steroidal anti-inflammatory drugs and corticosteroids. The mechanism of action of colchicine is to bind to the tubulin of neutrophils, thereby hindering the activity of granulocytes and inhibiting granulocyte infiltration. Non-steroidal anti-inflammatory drugs such ...
Claims
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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K9/48A61K9/20A61P19/06
CPCA61K31/352A61K9/2059A61K9/4866
Inventor 田丽华
Owner ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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