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A kind of drug coating and preparation method thereof

A drug coating and drug technology, applied in the field of medical devices, can solve the problems of drug coating phase separation, low bioavailability, drug coating loss, etc., to reduce shedding and loss, promote cell aggregation and growth, Promotes the repair of damaged mucosa

Active Publication Date: 2021-09-21
QINGDAO BIOTECH MEDICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The water-soluble small molecule carrier has the following disadvantages: first, because the molecular weight of the water-soluble small molecule is small (<1000D), the mechanical strength of the coating is weak, the film-forming effect is poor, and the affinity with the balloon surface is poor, and the drug coating The binding force between the layer and the balloon is weak, and the drug is prone to serious shedding and loss during the delivery process to the target lesion, which affects the consistency of the drug transfer amount during the full contact between the balloon and the lesion, and easily forms an "empty window". "area (the drug coating is completely lost in some areas on the surface of the balloon), which affects the clinical treatment effect
Second: Since the molecular weight of the water-soluble small molecule carrier is often the same order of magnitude or even smaller than that of the drug, in the case of a large difference in hydrophilicity between the carrier molecule and the drug (the HLB value of the water-soluble small molecule is often >10), it is easy to cause The phase separation phenomenon occurs in the drug coating, the drug dispersion effect is not good, the coating uniformity is poor, and the process stability control is difficult in large-scale production
Third, water-soluble small molecules are transferred to the mucosal surface with weak adhesion strength, short adhesion time, easy to be washed away or dissolved by blood or tissue fluid, difficult to achieve long-term drug release effect, and low bioavailability

Method used

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  • A kind of drug coating and preparation method thereof
  • A kind of drug coating and preparation method thereof
  • A kind of drug coating and preparation method thereof

Examples

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preparation example Construction

[0074] The embodiment of the present invention also discloses a preparation method of a drug coating, comprising the following steps:

[0075] (A) dissolving a biodegradable polymer with an amino group or a protonated amino group in a first solvent to obtain a first solution, and coating the first solution on the surface of the medical device to form a bottom layer;

[0076] (B) Coating a solution containing drugs, non-ionic water-soluble compounds and degradable polymers with carboxyl or carboxylate groups on part of the surface of the bottom layer to form a surface layer.

[0077] According to the present invention, step (A) dissolves the biodegradable polymer with amino group or protonated amino group in the first solvent to obtain the first solution, and coats the first solution on the surface of the medical device to form the bottom layer .

[0078] The first solvent is preferably one or more of acetone, tetrahydrofuran, methanol, ethanol, isopropanol, N,N-dimethylacetam...

Embodiment 1

[0124] a, bottom layer solution preparation: 0.5g chitosan quaternary ammonium salt (Mn=250000D), dissolve in 15mL deionized water, then magnetically stir at 50°C for 60 minutes until fully dissolved, add 5mL methanol to the deionized aqueous solution to prepare a mixture The solution was left to stand for 24 hours before use.

[0125] b. Preparation of surface layer solution: the first component, 0.5g of sodium hyaluronate (Mn=45000D), was dissolved in 10ml of deionized water, magnetically stirred at room temperature for 60 minutes until completely dissolved, and 10mL of ethanol was added to the deionized aqueous solution to prepare a mixed solution Stand still for 24 hours for use; the mixture of the second component 0.0875g glycerin and the third component 0.25g paclitaxel (purity > 95%) was dissolved in 10mL ethanol solution, magnetically stirred at room temperature for 30 minutes until completely dissolved, and added to ethanol Add 10mL deionized water to the solution to ...

Embodiment 2

[0128] a, bottom solution preparation: 0.5g hydroxypropyl chitosan (Mn=300000D), be dissolved in 8mL deionized water, magnetically stir at normal temperature for 60 minutes to dissolve completely, add 2mL ethanol in deionized water and prepare to mix The solution was left to stand for 24 hours before use.

[0129] b. Preparation of degradable polymer mixed solution: first component 0.65g polylactic acid-glycolic acid copolymer (Mn=14000D), second component 0.1g rhamnosyl ester (content > 85%; monorhamnosyl ester Content > 50%), the third component 0.05 pyridine carboxamide mixture was dissolved in 30ml of tetrahydrofuran and deionized water mixed solution (tetrahydrofuran: deionized water = 2:1), 40 ℃ environment until completely dissolved and let stand for 24 hours stand-by;

[0130] c. Drug solution preparation: the first component 0.35g rapamycin (purity > 95%) and the second component 0.015g vitamin C mixture were dissolved in 10ml ethanol, magnetically stirred at room te...

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Abstract

The invention relates to a drug coating, comprising: a bottom layer, the bottom layer includes biodegradable polymers with amino groups or protonated amino groups; the bottom layer is arranged on the surface of medical devices; Sexual compounds and degradable polymers with carboxyl or carboxylate groups; the surface layer is coated on the surface of the bottom layer and does not completely cover the bottom layer; drugs, the drugs are only contained in the surface layer or contained in the bottom layer at the same time and in the surface layer. The drug coating has a strong binding force with the surface of the medical device, which can effectively reduce drug loss during device delivery, improve the transfer amount, consistency and retention time of the drug to the mucosa, prolong the drug release period, and improve bioavailability. At the same time, the drug coating can activate the coagulation effect at the bleeding site in the injured area, which is conducive to the adhesion and growth of cells in the injured area, and promotes healing.

Description

technical field [0001] The invention relates to the field of medical devices, in particular to a drug coating and a preparation method thereof. Background technique [0002] It is becoming more and more to treat various medical diseases by implanting or intervening medical devices into the vascular and luminal system of the patient's body. In particular, it is more and more common to use medical devices to treat local diseases with targeted drugs, such as drug stents, drug balloon catheters, etc. [0003] In the past few years, a large number of medical devices carrying drugs have been developed, among which drug stents are currently one of the most commonly used and most effective drug-containing medical devices. The stent is mixed with a drug and a polymer matrix and coated on the surface of the stent to form a local slow drug release system. When the stent is implanted in the blood vessel, esophagus, biliary tract or other lumens, the drug will be slowly released for sev...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61L29/16A61L29/08A61L31/16A61L31/10
CPCA61L29/085A61L29/16A61L31/10A61L31/16A61L2300/216A61L2300/606A61L2420/02A61L2420/08C08L5/08C08L67/04C08L77/02C08L71/02C08L29/04
Inventor 孙燕魏彦
Owner QINGDAO BIOTECH MEDICAL CO LTD
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