New uses of amlexanox

An amlenoxanol and application technology, applied in medical preparations, prostheses, catheters and other directions containing active ingredients, can solve the problems of weakening the long-term efficacy of anti-restenosis, incomplete and other problems, achieve inhibition of smooth muscle cell proliferation, prevent Restenosis, the effect of preventing the incidence of vascular restenosis

Active Publication Date: 2020-04-10
MICROPORT SINICA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the application of DES has effectively reduced the incidence of restenosis in the short term after surgery, studies have shown that while DES inhibits the proliferation of vascular smooth muscle cells, it also delays endothelial repair, thereby causing cardiovascular diseases such as incomplete stent intima and thrombosis. Adverse events, ultimately weakening the long-term efficacy of anti-restenosis

Method used

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  • New uses of amlexanox

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0060] Experimental Example 1: Cell Experiment

[0061] A drug preparation:

[0062] (1) Amlexanox configuration:

[0063] a) Before the experiment, the drug stent loaded with amlexanox was placed in DMSO solution, and after it was completely dissolved, it was further diluted to form a drug concentration of 10 -2 mmol / ml solution.

[0064] b) add 10 -2 The drug solution of mmol / ml was diluted with dimethyl sulfoxide (DMSO) to a concentration of 10 -3 ,10 -4 ,10 -5 , 10 -6 ,10 -7 ,10 -8 ,10 -9 mmol / ml drug solution.

[0065] c) After dispensing the series of concentration drug solutions prepared above, store them temporarily at -20 degrees Celsius for later use.

[0066] d) When in use, dilute the stored DMSO for 10 -2 ~10 -9 After the drug solution was taken out and returned to normal temperature, the drug solution of each concentration was diluted 1000 times with the corresponding complete cell culture medium to carry out the cell test, that is, the final use con...

Embodiment 2

[0094] Embodiment 2 drug-eluting stent

[0095] Mix 300mg of amlexanox (drug) and 300mg of PLGA (drug carrier) in 20ml of chloroform. After the solute is completely dissolved, spray the solution evenly on the surface of the L605 cobalt-chromium alloy metal stent by ultrasonic atomization until the drug is loaded. The amount reaches 50μg / cm 2 . The drug-eluting stent is prepared after the solvent is completely evaporated at room temperature.

Embodiment 3

[0096] Example 3 Nanoporous preloaded drug type

[0097] Fine lines are formed on the surface of the stainless steel stent body through friction treatment, the micronized amlexanox and the stent body are placed in a high-pressure airtight device, and the device is turned on, so that the drug particles are embedded in the fine lines of the stent body , to be loaded to reach 50μg / cm 2 , to obtain a drug-eluting stent.

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Abstract

The present invention relates to the use of amlexanox or its salt or its solvate in the preparation of a drug with smooth muscle cell inhibitory effect, especially the use of the drug for preventing and treating vascular restenosis. The invention also relates to the technical field of medical instruments. The medical device, especially the drug stent, distributes amlexanox or its salt or its pharmaceutical composition on the surface. The present invention has discovered a brand-new biological activity of amlexanox, which has a high activity of inhibiting the proliferation of smooth muscle cells. Compared with the currently commonly used smooth muscle cell proliferation inhibitors, it also has a low inhibitory effect on endothelial cell growth. Features, especially suitable for medical devices, while preventing the incidence of vascular restenosis, it will not delay endothelial repair, so it can shorten the time for patients to take antithrombotic and platelet drugs after surgery, and greatly improve the long-term efficacy.

Description

technical field [0001] The present invention relates to the use of amlexanox or its salt or its solvate in the preparation of a drug with smooth muscle cell inhibitory effect, especially the use of the drug for preventing and treating vascular restenosis. [0002] The invention also relates to the technical field of medical devices. Background technique [0003] Amlexanox (Amlexanox) common name: 2-amino-7-isopropyl-5-oxo-5H[1]phenylpyranyl-[2,3,-b]-pyridine-3-carbonic acid di Toluic acid, also known as CHX3673. English chemical name: 2-amimo-7-isopropyl-5-oxo-5H-[1]benzopyrano-[2,3,-b]pyridine-3-carboxylic acid. Amlexanox is an allergic reaction mediator blocker, which stabilizes the cell membrane of mast cells and inhibits their degranulation, thereby preventing the release of allergic reaction mediators and exerting an anti-allergic effect. It was first launched in Japan in 1987 for the treatment of allergic bronchial asthma. Later applied to allergic rhinitis. In 19...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/436A61P9/00A61P9/10A61L27/54A61L29/16A61L31/16
CPCA61L27/54A61L29/16A61L31/16A61K31/436A61L2300/204A61L2300/416A61P9/00A61P9/10A61K45/06A61K2300/00
Inventor 陈陆李俊菲陈飞成晓
Owner MICROPORT SINICA CO LTD
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