Percutaneous absorption preparations

An absorption type and preparation technology, which is applied in the field of percutaneous absorption type dementia treatment preparations, can solve problems such as side effects of the digestive tract, influence on liver function, and difficulty in treatment effect

Inactive Publication Date: 2005-01-26
HISAMITSU PHARM CO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The reason is that it is generally difficult to avoid the first-pass effect in the liver of oral drugs, so it is easy to affect liver function. In addition, the presence of high concentrations in the digestive tract leads to side effects on the digestive tract
In the case of an oral drug, the ratio (A / B) is relatively large, therefore, if the concentration in plasma does not reach the concentration where side effects are found, it will be difficult to maintain long-term therapeutic effect

Method used

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  • Percutaneous absorption preparations
  • Percutaneous absorption preparations
  • Percutaneous absorption preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] (prescription)

[0069] SIS 17.1%

[0070] PIB 7.3%

[0071] Alicyclic saturated hydrocarbon resin (Arkon P100) 41.6%

[0072] Liquid paraffin 29.4%

[0073] Sodium acetate 0.6%

[0074] Donepezil Hydrochloride 1.0%

[0075] Pyrothiodecane 3.0%

[0076] Total 100.0%

[0077] Donepezil hydrochloride, sodium acetate, pyrothiodecane, and liquid paraffin were put in a mortar in advance, mixed well, and then mixed with the remaining components dissolved in toluene. After it is coated on release paper, it is dried to remove the solvent, and then bonded to a PET film support to obtain the percutaneous absorption preparation of the present invention.

Embodiment 2

[0079] (prescription)

[0080] SIS 16.6%

[0081] Acrylic polymer 7.0%

[0082] (Duro.Tak87.2287, National Starch and Chemical Company)

[0083] Alicyclic saturated hydrocarbon resin (Arkon P100) 40.2%

[0084] Liquid paraffin 28.4%

[0085] Sodium acetate 1.8%

[0086] Donepezil Hydrochloride 3.0%

[0087] Pyrothiodecane 3.0%

[0088] Total 100.0%

[0089] Donepezil hydrochloride, sodium acetate, pyrothiodecane, and liquid paraffin were put in a mortar in advance, mixed well, and then mixed with the remaining components dissolved in toluene. After it is coated on release paper, it is dried to remove the solvent, and then bonded to a PET film support to obtain the percutaneous absorption preparation of the present invention.

Embodiment 3

[0091] (prescription)

[0092] SIS 16.0%

[0093] PIB 6.8%

[0094] Alicyclic saturated hydrocarbon resin (Arkon P100) 38.8%

[0095] Liquid paraffin 27.4%

[0096] Sodium acetate 3.0%

[0097] Donepezil Hydrochloride 5.0%

[0098] Sorbitan Monolaurate 3.0%

[0099] Total 100.0%

[0100] Donepezil hydrochloride, sodium acetate, sorbitan monolaurate, and liquid paraffin were previously placed in a mortar and mixed well, and then mixed with the remaining components dissolved in toluene. After it is coated on release paper, it is dried to remove the solvent, and then bonded to a PET film support to obtain the percutaneous absorption preparation of the present invention.

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Abstract

Percutaneous absorption preparations for treating dementia which contain an adhesive composition, characterized in that the adhesive composition contains the active ingredient in a dispersed state, the active ingredient is released at a pharmacologically effective rate and the skin permeation rate thereof is at least 1.2 mug / cm<2> / h. Thus, it is possible to provide percutaneous absorption preparations whereby the therapeutic effect can be sustained over a prolonged period of time without elevating the concentration of the active ingredient in the plasma to such a level as causing the expression of side effects in the administration of remedies for dementia.

Description

technical field [0001] The invention relates to a percutaneous absorption type dementia treatment preparation, in particular to a percutaneous absorption type preparation of donepezil, icopezil, Zanapezil, ER-127528 and other treatment agents for Alzheimer type dementia. Background technique [0002] Donepezil is an acetylcholinesterase (AChE) inhibitor and is currently clinically used as a therapeutic agent for Alzheimer's type dementia. For Alzheimer's dementia with reports of cholinergic nervous system disorders in the brain, AChE blockers such as donepezil can increase acetylcholine in the brain and activate the cholinergic nervous system in the brain. The currently used formulation of donepezil is a tablet, which is prescribed orally to patients with Alzheimer's type dementia. [0003] With the current further development of therapeutic drugs for Alzheimer's dementia, as compounds having the same AChE blocking effect, ER-127528 represented by the following formula, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/00A61K31/445A61K47/10A61K47/12A61K47/16A61K47/18A61K47/26A61P25/28
CPCA61K47/16A61K31/00A61K9/7053A61K9/7061A61K47/26A61K31/445A61K9/0014A61K47/12A61K47/10A61K47/18A61K9/7076A61P25/28A61P43/00A61K9/70
Inventor 寺原孝明利光新太上村谦吾肥后成人后藤武佐藤秀次
Owner HISAMITSU PHARM CO INC
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