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Transdermal patch containing formoterol or fumarate thereof

A technology of transdermal patch and fumarate, which is applied in the field of medicine, can solve the problems of the stability of formoterol and the limitation of the ability to improve transdermal permeability, and achieve good transdermal permeability and good stability. Effect

Active Publication Date: 2015-12-16
DALIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to ensure the adhesive performance of the patch, the content of the pressure-sensitive adhesive in the patch is not less than 40%wt, and the cationic polymer as an additive is limited to 20%wt, so the matrix has a great influence on the stability and transdermal properties of formoterol. The ability to increase permeability is somewhat limited

Method used

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  • Transdermal patch containing formoterol or fumarate thereof
  • Transdermal patch containing formoterol or fumarate thereof
  • Transdermal patch containing formoterol or fumarate thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: wherein 1-1 to 1-10 are comparative prescriptions, and 1-11 to 1-14 are embodiments of the present invention.

[0029]

[0030]

[0031] The specific preparation method is as follows: weigh formoterol, add methanol and stir for 20-30 minutes to completely dissolve the formoterol to form a drug solution. Add pressure-sensitive adhesive and related auxiliary materials and stir evenly. After degassing, apply the prepared drug-loaded pressure-sensitive adhesive matrix solution on the anti-adhesive film treated with silicone resin. After drying, cover it with a film on the surface of the lining material. Molded into products.

Embodiment 2

[0032] Embodiment 2: 2-1 to 2-8 are all embodiments of the present invention.

[0033]

[0034]

[0035] Specific preparation process: Weigh formoterol fumarate or formoterol, add methanol and stir for 20-30 minutes to completely dissolve to form a drug solution. Add auxiliary materials such as penetration enhancer, add pressure-sensitive adhesive and stir thoroughly for 1 hour to obtain a uniform drug-containing glue. The glue is coated on the anti-adhesive layer, dried and pressed to cover the backing layer, and the product is formed by stamping.

Embodiment 3

[0037] Select above-mentioned several kinds of pressure-sensitive adhesive patches containing 1%wt formoterol, adopt acrylic pressure-sensitive adhesives containing other functional groups and prepare comparative preparations with existing patented technical schemes, and prepare formoterol transdermal patches The agent is carried out in vitro transdermal test comparative study, and the specific preparation method is the same as in Example 1, and its performance results are as follows (see figure 1 and Table 1):

[0038] Table 1: Comparison of chemical composition and functional groups of pressure-sensitive adhesives.

[0039]

[0040]

[0041] O: Adhesion is good, and there is no stringing phenomenon in the 24-hour penetration test.

[0042] X: Adhesion is poor, cohesion is insufficient, and stringing occurs after the test.

[0043] Among them, in Comparative Examples 1-1 to 1-8, the pressure-sensitive adhesive does not contain amino groups, the percutaneous permeabili...

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Abstract

The invention provides a transdermal patch containing formoterol or fumarate thereof. The transdermal patch is composed of a lining layer, a drug-carrying pressure sensitive layer and an anti-adhesion layer, the drug-carrying pressure sensitive layer is composed of a pressure sensitive adhesive and formoterol or fumarate thereof, content of formoterol or fumarate thereof, in percentage by mass is 1-10%, and a drug-carrying matrix is an acrylate pressure-sensitive adhesive containing amino. By a system, stability and percutaneous permeability of formoterol can be improved effectively, and the problem of long delay time of formoterol is reduced; the patch prepared by using the pressure-sensitive adhesive system is high in physical stability, and adhesion performance of the patch is maintained good after additives like a permeation promoter are added. The transdermal patch has the advantages that the patch has excellent stability, high percutaneous permeation rate and long continuous administration time, can meet requirements on administration once every day or several days and can effectively prevent and treat asthma.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a beta 2 The transdermal drug delivery system of receptor agonist formoterol specifically refers to a transdermal patch containing formoterol or its fumarate, which can be used for the treatment of asthma and other diseases. Background technique [0002] Asthma (bronchial asthma) is a common and multiple airway chronic respiratory disease involving a variety of cells (eosinophils, T lymphocytes, neutrophils, airway epithelial cells, etc.) and cell components. And cause recurrent symptoms such as wheezing, shortness of breath, chest tightness or coughing, often at night and / or in the early morning. Asthma is an important disease that affects people's physical and mental health. If the treatment is not timely and standardized, asthma can be fatal. The approach to asthma treatment is to use long-acting controller medications to maintain control of persistent asthma, and rapid-reli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/137A61K31/205A61K47/32A61P11/06
Inventor 汪晴李晓晖张长青
Owner DALIAN UNIV OF TECH
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