Percutaneous absorption preparation

A preparation and cross-linking agent technology, applied in the field of percutaneous absorption preparations, can solve the problems of insufficient prevention of cohesive failure of the adhesive layer, cohesive failure of the edge, whitening of the adhesive layer, etc., and achieve stable skin irritation , Suppresses the reduction of cohesive force, excellent sticky effect

Inactive Publication Date: 2009-10-28
NITTO DENKO CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, in the former method (Patent Document 3), since the polyol compound is a hydrophilic compound, when the adhesive layer is used in a hydrophobic environment, the concentration at which the polyol compound is uniformly dissolved is only about 5% by weight at most. When the concentration is higher than the above, it may cause whitening of the adhesive layer
Therefore, when a large amount of basic drug is contained in the adhesive layer, the content of the polyol compound that is uniformly dissolved in the adhesive layer is further reduced, and the cohesive failure of the adhesive layer may not be sufficiently prevented.
In addition, it is also considered to increase the content of the polyol compound in the adhesive layer. In this case, since the content of the adhesive in the adhesive layer decreases, the adhesive force may decrease.
In addition, although the latter method (Patent Document 4) can suppress the cohesive failure of the sticking surface at the time of peeling off, when the side of the edge portion of the percutaneous absorption preparation contacts the skin during sticking, cohesion in the edge portion may be caused. destroy

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0090] Acrylic adhesive solution A containing 51 parts of adhesive solid content, 40 parts of isopropyl myristate, and 8 parts of donepezil were mixed and stirred in a container to make them uniform. After that, further add 1 part of sodium chloride dispersed in ethanol with a primary particle size of about 10 μm and a secondary particle size of about 50 μm, stir, and then add 0.4 parts of sodium chloride per 100 parts of binder solid content. Add ethyl acetoacetate aluminum diisopropoxide in a small amount, adjust the viscosity with ethyl acetate, apply the liquid on a PET film (75 μm thick) to a thickness of 60 μm after drying, and dry to form an adhesive layer. It was pasted on a PET film (thickness 12 μm) after silicone release treatment, and subjected to aging treatment (crosslinking treatment of the adhesive layer) at 70° C. for 48 hours to obtain a transdermal preparation of donepezil.

Embodiment 2

[0092] Except that the amount of acrylic adhesive solution A is changed to 49 parts of the solid content of the adhesive, and the amount of sodium chloride dispersed in ethanol is changed to 3 parts, the same as in Example 1 Operation, obtain the percutaneous absorption preparation of donepezil.

Embodiment 3

[0094] Except that the amount of the acrylic adhesive solution A is changed to the amount that the solid content of the adhesive is 47 parts, and the amount of sodium chloride dispersed in ethanol is changed to 5 parts, the same operation as in Example 1 , to obtain a transdermal preparation of donepezil.

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PUM

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Abstract

The present invention provides a percutaneously absorbable preparation for percutaneous absorption of donepezil or its hydrochloride which is stable and resistant to loss of cohesiveness of the pressure-sensitive adhesive layer while attached and resistant to adhesive transfer due to cohesive failure during removal by peeling. The percutaneously absorbable preparation comprises 2-[(1-benzyl-4-piperidinyl)methyl]-5,6-dimethoxyindan-1-on and / or its hydrochloride and a metal chloride in a pressure-sensitive adhesive layer which has been crosslinked.

Description

technical field [0001] The present invention relates to a compound containing 2-[(1-benzyl-4-piperidinyl)methyl]-5,6-dimethoxyindan-1-one (hereinafter also referred to as "Donepezil (Donepezil)" ) and / or 2-[(1-benzyl-4-piperidinyl)methyl]-5,6-dimethoxyindan-1-one monohydrochloride (hereinafter also known as "donepezil hydrochloride") for transdermal absorption. More specifically, the present invention relates to a percutaneous absorption preparation that sticks to the surface of the skin and continuously administers the above-mentioned drug into the body from the skin. Background technique [0002] Donepezil as a basic drug or donepezil hydrochloride as its hydrochloride has an acetylcholinesterase inhibitory effect and can be used as an anti-Alzheimer's type dementia drug. Patients with Alzheimer's disease type dementia are mostly elderly people, and it is often difficult for elderly people to swallow oral preparations. In addition, patients who develop symptoms of Alzhe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/445A61K9/70A61K47/02A61K47/14A61K47/32A61P25/28
CPCA61F2013/00646A61K31/445A61K9/7061A61P25/28A61K9/70A61K47/02
Inventor 花谷昭德和城智子明见仁
Owner NITTO DENKO CORP
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