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Transdermally absorbable donepezil-containing preparation

A donepezil and absorption-type technology, which is applied in the direction of medical preparations containing active ingredients, medical preparations with inactive ingredients, organic active ingredients, etc., can solve the problem of insufficient and difficult to take anti-dementia drugs, drug percutaneous absorption Increased blood drug concentration and other problems to achieve the effect of avoiding side effects, reducing side effects, and effective treatment

Active Publication Date: 2012-07-11
TEIKOKU SEIYAKU KK TEIKOKU SEIYAKU CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, for dementia patients whose symptoms have worsened, it is difficult to take anti-dementia drugs in many cases
As a dosage form suitable for such a situation, Patent Document 1 describes a transdermal preparation containing donepezil and a suppository, but the invention is mainly related to an ointment, a cream, or a suppository, and it is not possible to continuously administer the active ingredient for a long time
[0004] In addition, Patent Document 2 describes an ointment containing donepezil, which is characterized in that the transdermal rate is at least 1.2 μg / cm 2 / hr or more, but since the active ingredient is dispersed and compounded in the patch, it is not sufficient for the percutaneous absorption of the drug, especially the rapid increase in the blood concentration after administration.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] (prescription)

[0088] SIS 15%

[0089] Liquid Paraffin 24%

[0090] BHT 1%

[0091] Glycerides of Hydrogenated Rosin 35%

[0092] Triacetin 5%

[0093] Donepezil 20%

[0094] Total 100%

[0095] After previously dissolving donepezil in a mixture of triacetin and toluene, mix with the remaining ingredients dissolved in toluene. After the mixture was coated on a release film, the toluene was dried and removed, and then bonded to a PET film backing layer to obtain the transdermal preparation of the present invention.

Embodiment 2～ Embodiment 10

[0097] According to the compounding shown in Table 1 below, the transdermal preparations of Examples 2 to 10 of the present invention were obtained according to the method described in Example 1 above.

[0098] 【Table 1】

[0099]

Embodiment 11～ Embodiment 21

[0104] According to the compounding shown in the following table 2, the compounding amount of donepezil and the compounding amount of triacetin, lauromacrogol, and lauryl alcohol as the absorption enhancer are changed, and the method of embodiment 1 is obtained according to the method of embodiment 1. 11 to the percutaneous absorption type preparation of Example 21.

[0105] 【Table 2】

[0106]

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PUM

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Abstract

Disclosed is a transdermally absorbable donepezil-containing preparation which enables the administration of donepezil in a sustained manner for a long period and can achieve both the rapid increase in blood donepezil level and the sustained release of donepezil. The transdermally absorbable donepezil-containing preparation comprises an adhesive patch base material comprising a hydrophobic polymer and an absorption-enhancing agent and donepezil (an active ingredient) dissolved in the adhesive patch base material, wherein the absorption-enhancing agent comprises at least one component selected from lauryl alcohol, triethyl citrate, isopropyl myristate, cetyl lactate, oleyl alcohol, sorbitan monooleate, polyethylene glycol monostearate, lauromacrogol, N-methyl-2-pyrrolidone and triacetin.

Description

technical field [0001] The present invention relates to a transdermal preparation having a backing layer (support) and an adhesive layer containing an adhesive matrix and a drug. Specifically, the drug contained as an active ingredient is donepezil (donepezil) used for the treatment of dementia. ) percutaneous absorption type preparation of an anti-dementia therapeutic agent. Background technique [0002] Donepezil has an acetylcholinesterase inhibitory activity and is widely used as a therapeutic drug for so-called Alzheimer's disease, which can suppress the exacerbation of symptoms of Alzheimer's disease. In Alzheimer's disease in which a disorder of the cholinergic nervous system in the brain has been reported, an acetylcholinesterase inhibitor such as donepezil increases acetylcholine in the brain and activates the cholinergic nervous system in the brain. Currently, preparations of donepezil for practical use are known as preparations for oral administration such as tab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/445A61K9/08A61K9/70A61K47/10A61K47/14A61K47/22A61K47/34A61P25/28
CPCA61K31/445A61K9/7053A61P25/28A61K9/7061
Inventor 川上智山地正博
Owner TEIKOKU SEIYAKU KK TEIKOKU SEIYAKU CO LTD
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