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Compound teriflunomide transdermal patch for treating rheumatic arthritis, and preparation method thereof

A teriflunomide transdermal patch, teriflunomide transdermal technology, applied in the field of medicine, can solve the problems of poor transdermal permeability, limit transdermal application, etc., achieve good flexibility, improve transdermal penetration Overdose, long-lasting and stable effect

Active Publication Date: 2014-01-22
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, TEF and most non-steroidal anti-inflammatory drugs (such as Oxicam NSAIDs) are weakly acidic drugs with poor transdermal permeability, which limits their transdermal application

Method used

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  • Compound teriflunomide transdermal patch for treating rheumatic arthritis, and preparation method thereof
  • Compound teriflunomide transdermal patch for treating rheumatic arthritis, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Disperse 2.8g of teriflunomide and 1.95g of lornoxicam in 100g of absolute ethanol, mix the two mixed solutions with 100g of acrylic pressure-sensitive adhesive, and spread them evenly on the release layer , dried at 50°C for 15 minutes, then compounded with a backing material including PVC or non-woven fabric, punched out to a certain size and specification, and the product is ready.

Embodiment 2

[0032] Take 2.8g of teriflunomide and dissolve or evenly disperse in 32g of acetone, dichloromethane, chloroform, ethanol, ether or ethyl acetate solvent, and slowly add in diethylamine with equimolar amount of teriflunomide solution under stirring , stirred at room temperature under condensing and reflux conditions, teriflunomide was completely dissolved, continued to stir for 1.5-3 hours, and removed the solvent by rotary evaporation to obtain teriflunomide diethylamine salt for later use;

[0033] Get 1.95g of lornoxicam and dissolve or evenly disperse in 32g of acetone, dichloromethane, chloroform, ethanol, ether or ethyl acetate solvent, slowly add in the diethylamine of equimolar amount with lornoxicam under stirring , stirred at room temperature under condensing and reflux conditions, lornoxicam was completely dissolved, continued to stir for 1.5-3 hours, and removed the solvent by rotary evaporation to obtain lornoxicam diethylamine salt for subsequent use;

[0034] Th...

Embodiment 3

[0036] Take 2.7g of teriflunomide and dissolve or evenly disperse it in 34g of acetone, dichloromethane, chloroform, ethanol, ether or ethyl acetate solvent, slowly add in the triethylamine of equimolar amount with teriflunomide solution under stirring , stirred at room temperature under condensing and reflux conditions, teriflunomide was completely dissolved, continued to stir for 1.5-3 hours, and removed the solvent by rotary evaporation to obtain teriflunomide triethylamine salt for subsequent use;

[0037] Get 2g of lornoxicam and dissolve or evenly disperse in 30g of acetone, dichloromethane, chloroform, ethanol, ether or ethyl acetate solvent, slowly add in the triethylamine of equimolar amount with lornoxicam under stirring, Stir at room temperature under condensing and reflux conditions, lornoxicam is completely dissolved, continue to stir for 1.5-3 hours, and remove the solvent by rotary evaporation to obtain lornoxicam triethylamine salt for subsequent use;

[0038] ...

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PUM

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Abstract

The invention discloses a compound teriflunomide transdermal patch for treating rheumatic arthritis, and a preparation method thereof, and belongs to the technical field of medicines. The compound teriflunomide transdermal patch for treating rheumatic arthritis is composed of a back lining layer, a medicine storage layer and an anti-adhesive layer, wherein the medicine storage layer is mainly prepared from the following raw material drugs in parts by weigh: 0.55-12 parts of teriflunomide, 0.55-12 parts of non-steroid anti-inflammatory drug, and 100 parts of pressure-sensitive adhesive. The compound teriflunomide transdermal patch can be used for avoiding irritation of an oral drug to gastrointestinal tracts, increasing the percutaneous permeability of the drug by an ion-pair technology, has a durable and stable curative effect, and can be used for treating rheumatic arthritis and pains caused by the same; if administration is interrupted, the patch can be peeled off, and the use is convenient; the patch is good in adhesion and flexibility.

Description

technical field [0001] The invention relates to a compound teriflunomide transdermal patch for treating rheumatoid arthritis and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Rheumatoid arthritis is a long-term chronic inflammation caused by an autoimmune disorder that causes the immune system to attack the joints. The disease is prone to occur in small joints such as hands, wrists, and feet, and recurs in a symmetrical distribution. This inflammation can cause irreversible joint damage to disability, and can lead to joint degenerative changes due to joint pain and wear, so it is considered a locally aggressive tumor. Epidemiological studies have shown that the prevalence of rheumatoid arthritis is about 0.28%, and it gradually increases with age. The prevalence of middle-aged and elderly people over 46 years old is the highest, and the prevalence of women is 6 times that of men. . In my country, the prevalence o...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/277A61K45/00A61P19/02A61P29/00
Inventor 方亮奚宏磊
Owner SHENYANG PHARMA UNIVERSITY
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