Transdermal patch containing diclofenac epolamine and preparation method thereof

A technology of diclofenac epoamide and transdermal patch is applied in the field of diclofenac epoamide transdermal patch and preparation thereof, and can solve the problems of low bioavailability, low penetration rate of gel preparation and the like

Inactive Publication Date: 2016-08-24
NANJING HEALTHNICE MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Wherein diclofenac sodium is slightly soluble in water, diclofenac potassium and diclofenac diethylamine are slightly soluble in water, and their gel preparations have low transdermal rate and low bioavailability, so new formulations with high transdermal rate are needed.

Method used

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  • Transdermal patch containing diclofenac epolamine and preparation method thereof
  • Transdermal patch containing diclofenac epolamine and preparation method thereof
  • Transdermal patch containing diclofenac epolamine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Single-dose prescription composition

[0022]

[0023] Preparation:

[0024] ① Weigh the prescribed amount of diclofenac eporamide and ethyl paraben, add it to propylene glycol, stir until dissolved, and set aside; first add the prescribed amount to neutralize sodium polyacrylate, sodium carboxymethyl cellulose, calcium carbonate, titanium dioxide, Polysorbate 80, stir evenly, then add the prescribed amount of glyoxate, stir evenly;

[0025] ②Preheat the prescribed amount of purified water to 50°C±2°C, add the prescribed amount of gelatin, povidone K90 and stir until dissolved, add the prescribed amount of edetate disodium and sorbitol, stir until dissolved, and keep warm;

[0026] ③Add the tartaric acid of the prescribed amount into the purified water according to the concentration (w / v) of 1.9%, and set aside;

[0027] ④ Slowly add the solution ② into the drug-containing solution ①; add the solution ③, and stir in vacuum for 3 minutes to obtain the drug-containin...

Embodiment 2

[0031] Single-dose prescription composition

[0032]

[0033] Preparation method: with embodiment 1.

Embodiment 3

[0035] Single-dose prescription composition

[0036]

[0037] Preparation method: with embodiment 1.

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PUM

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Abstract

The invention provides a transdermal patch containing diclofenac epolamine and its preparation method. The transdermal patch contains the following ingredients (by weight): 0.5-5.0% (preferably 1.3%) of diclofenac epolamine which is used as a main active ingredient, 1-10% of a skeleton agent, 15-25% of a wetting agent, 0-0.5% of a complexing agent, 0-10% of an adhesive, 0-1% of a whitening agent, 0-1% of a skin penetration enhancer, 0-1% of a bacteriostat, 0-1% of a crosslinking regulator, etc. and the rest of purified water. in the preparation, dihydroxyaluminium aminoacetate is selected as the crosslinking regulator, and ethylparaben is selected as the bacteriostat. The diclofenac epolamine transdermal patch prepared by the technology has more stable quality, is convenient to use, has a simple preparation process and is suitable for large-scale production.

Description

technical field [0001] The invention relates to a diclofenac eporamide transdermal patch and a preparation method thereof, belonging to the technical field of medicinal chemistry. Background technique [0002] The chemical name of diclofenac eporamide is 2-[(2,6-dichlorophenyl)amino]phenylacetic acid 2-pyrrolidine ethanolate, and the molecular formula is C 20 h 24 Cl 2 N 2 o 3 , the molecular weight is 411.3, and the structural formula is: [0003] [0004] Diclofenac Eporamide Patch was developed by the Swiss company IBSA and launched in the United States in 2008. [0005] Diclofenac eporamide is a non-steroidal anti-inflammatory drug (NSAIDs), and its active ingredient diclofenac is a derivative of phenylacetic acid, which has significant analgesic and anti-inflammatory effects. Diclofenac inhibits the biosynthesis of prostaglandins, which are major contributors to inflammation, pain, and fever. [0006] Diclofenac Eporamide can be used to relieve mild to moderat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/40A61P29/00
Inventor 张蓓蓓邹巧根
Owner NANJING HEALTHNICE MEDICAL TECH
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