Uses of pi3k/mtor dual inhibitors

A dual inhibitor and inhibitor technology, applied in the field of medical devices, can solve the problem of high stenosis rate, achieve the effect of reducing the rate of vascular restenosis, inhibiting vascular intimal hyperplasia, and having a strong effect

Active Publication Date: 2020-08-25
MICROPORT SINICA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The purpose of the present invention is to provide a PI3K / mTOR dual inhibitor in the preparation of drugs for inhibiting intimal hyperplasia, a drug-loaded stent and a preparation method thereof, so as to solve the problem that the restenosis rate is still relatively high after implanting a drug-eluting stent in a patient. high problem

Method used

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  • Uses of pi3k/mtor dual inhibitors
  • Uses of pi3k/mtor dual inhibitors
  • Uses of pi3k/mtor dual inhibitors

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0063] Experimental Example 1: Cell Experiment

[0064] A drug preparation:

[0065] a) Before the experiment, the drug stents loaded with different PI3K / mTOR dual inhibitors were placed in DMSO solution, completely dissolved and further diluted to form a drug concentration of 10 -2 mmol / ml solution.

[0066] b) add 10 -2 The drug solution of mmol / ml was diluted with DMSO to a concentration of 10 -3 ,10 -4 ,10 -5 …10 -9 mmol / ml drug solution.

[0067] c) After dispensing the series of concentration drug solutions prepared above, store them temporarily at -20 degrees Celsius for later use.

[0068] d) When in use, dilute the stored DMSO for 10 -2 ~10 -9 After the rapamycin 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 concentrations were 10 -5 ,10 -6 ,10 -7 ,10 -8 ,10 -9 ,10 -10 ,10 -11 ,10 - ...

experiment example 2

[0094] Experimental example 2: Animal experiments

[0095] Research object A: select Bama miniature pigs, male, 1-2 months old, and feed them with induction feed formula for 5 months. The induction feed formula is: 30% sucrose, 15% butter, 3% cholesterol, 17% soybean cake, 5% fish meal, 20% corn, 5% wheat flour, and 5% pounded rice bran. Pigs with hyperglycemia, hyperinsulinemia, and early manifestations of diabetic nephropathy such as microalbuminuria, glycosuria and nephritis were selected as experimental subjects.

[0096] B experimental group

[0097] 1. Rapamycin stent group: animals were implanted with rapamycin-containing stents

[0098] 2. GEN477 stent group: animals were implanted with stents containing GEN477

[0099] 3. BKM120 stent group: animals were implanted with stents containing BKM120

[0100] 4. GEN477+rapamycin stent group: animals were implanted with stents containing GEN477+rapamycin

[0101] C stent implantation

[0102] Aspirin and clopidogrel wer...

Embodiment 1

[0114] Weigh BKM120 and polylactic acid at a weight ratio of 1:3, mix and dissolve in acetonitrile solution to make a solution with a solid content of 0.9%. After the solute (ie, BKM120 and polylactic acid) was completely dissolved, the solution was evenly sprayed on the surface of the L605 cobalt-chromium alloy metal stent by means of ultrasonic atomization. The drug-loaded stent containing BKM120 was prepared after the acetonitrile was completely volatilized at room temperature.

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Abstract

The invention provides use of a PI3K/mTOR dual inhibitor, a medicine carrying stent and a preparation method of the medicine carrying stent. The PI3K/mTOR dual inhibitor is used for preparing a medicine for inhibiting vascular intimal hyperplasia and is loaded to a stent body to form the medicine carrying stent for inhibiting the vascular intimal hyperplasia; the PI3K/mTOR dual inhibitor is capable of simultaneously inhibiting PI3K and mTOR and can play duel-target role of the single medicine; and compared with a pure mTOR inhibitor, the PI3K/mTOR dual inhibitor has the advantages that the effect of inhibiting vascular smooth muscles is relatively strong, the vascular intimal hyperplasia is effectively inhibited, and the restenosis rate of blood vessels is further decreased.

Description

technical field [0001] The invention relates to the technical field of medical devices, in particular to the use of a PI3K / mTOR dual inhibitor in the preparation of drugs for inhibiting vascular intimal hyperplasia, a drug-loaded stent and a preparation method thereof. Background technique [0002] The emergence of molecularly targeted drugs from the end of the 20th century to the beginning of the 21st century is a milestone event in the development of anticancer drug research. Among them, the development of PI3K inhibitors as antitumor drugs has always been a hot spot in the pharmaceutical industry. Among them, LY294002 and Wortmannin (Wortmannin) are the two earliest PI3K inhibitors. Although they have shown certain anti-tumor effects in vivo and in vitro, they have not been studied due to the skin and liver toxicity, solubility and stability. able to enter clinical trials. [0003] After more than 10 years of development, PI3K inhibitors are developing in a more specific...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61L31/10A61L31/16A61K45/00A61P35/00
CPCA61K45/00A61K45/06A61L31/10A61L31/16A61L2300/404A61L2300/41A61L2300/414A61L2300/416A61L2300/42A61L2300/428A61L2300/45
Inventor 陈陆李俊菲胡燕姚瑶
Owner MICROPORT SINICA CO LTD
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