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A technology of amlexanox, which is used in the field of anti-restenosis drugs, can solve the problems of weakening the long-term anti-restenosis effect and incompleteness, and achieve the effect of inhibiting the proliferation of smooth muscle cells, preventing restenosis, and promoting healing
Active Publication Date: 2018-04-03
MICROPORT SINICA CO LTD
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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
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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 Nano-microporous pre-loaded 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 invention relates to an application of amlexanox or salt thereof or a solvate thereof in preparing medicines having a smooth muscle cell inhibiting effect, in particular to an application in medicines for preventing and treating vascular restenosis. The invention also relates to the technical field of medical apparatuses. The amlexanox or the salt or the pharmaceutical composition thereof is distributed on the surface of the medical apparatus, in particular a drug stent. A completely new bio-activity of the amlexanox is discovered, exactly the amlexanox is high in activity of inhibiting smooth muscle cell proliferation; in comparison with currently common smooth muscle cell proliferation inhibitors, the amlexanox also has the characteristic of being low in performance of inhibiting endothelial cell growth; therefore, the amlexanox is especially applicable to medical apparatuses; and the amlexanox can prevent the vascular restenosis occurrence rate, and in addition, the amlexanox can prevent delay of endothelial repair; therefore, the time of taking anti-thrombus and antiplatelet medicines of a patient after an operation can be shortened, and a long-term curative effect can be greatly improved.
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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