Transdermal medicament delivery system containing donepezil compound, preparation and preparation method

A transdermal drug delivery system, the technology of donepezil, applied in the field of transdermal drug delivery systems, can solve the problems of poor compliance and high clinical dropout rate of AD patients

Active Publication Date: 2011-09-21
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above patents all need to be taken daily and for a long time, which cannot solve the shortcomings of poor compliance and high clinical drop-out rate of AD patients
Chinese patent CN101167697A discloses a long-acting sustained and controlled release composition of donepezil compound and its preparation method, but all of them are injection or oral preparations, which also have the above-mentioned defects

Method used

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  • Transdermal medicament delivery system containing donepezil compound, preparation and preparation method
  • Transdermal medicament delivery system containing donepezil compound, preparation and preparation method
  • Transdermal medicament delivery system containing donepezil compound, preparation and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] [Prescription] (based on 2000 tablets)

[0103] Donepezil 55g, hydrophobic skeleton matrix acrylic pressure-sensitive adhesive 895.5g, humectant propylene glycol 20g, transdermal penetration enhancer isopropyl myristate 20g, pH regulator triethanolamine 9g, bacteriostatic agent methylparaben 0.5g; Total: 1000g

[0104] Preparation:

[0105] Add donepezil and methylparaben to a mixed solution of 400 g of glacial acetic acid and dichloromethane (glacial acetic acid:dichloromethane=1:2, volume ratio) to dissolve, and stir at 5000 rpm for 0.5 hours to obtain a medicinal solution;

[0106] Add acrylic pressure-sensitive adhesive and isopropyl myristate to the above drug solution, mix well, then add propylene glycol, and stir at a speed of 10,000 rpm for 1 hour, mix and disperse to obtain drug-containing glue.

[0107] Finally, add triethanolamine to the drug-containing colloid, mix, disperse, and degas to obtain the drug-containing colloid.

[0108] Coat the drug-containi...

Embodiment 2

[0112] [Prescription] (based on 2000 tablets)

[0113] Donepezil hydrochloride 80g, hydrophilic polymer matrix sodium polyacrylate 60g, transdermal penetration enhancer azone 96g, humectant glycerin 150g, crosslinking agent aluminum oxide 5g, acidic pH regulator tartaric acid 2g, alkaline pH regulator III Ethanolamine 54g, antibacterial agent benzyl alcohol 3g; solvent water 550g; total: 1000g

[0114] Preparation method: add donepezil hydrochloride, benzyl alcohol and tartaric acid to water and dissolve to obtain medicinal solution A; put sodium polyacrylate and aluminum oxide together in glycerin to suspend and swell for 2 hours to obtain sodium polyacrylate suspension B ; Slowly add the medicinal solution A to the above-mentioned sodium polyacrylate suspension B, while stirring at a speed of 10000 rpm for 1 hour, mix and disperse to obtain a hydrogel solution. Then add azone to the above-mentioned hydrogel liquid, mix and disperse, finally add triethanolamine, adjust the p...

Embodiment 3

[0119] [Prescription] (based on 2000 tablets)

[0120] Donepezil hydrochloride 100g, solvent hydroalcoholic solution (water:ethanol=6:4, volume ratio) 200g, polyvinylpyrrolidone (K-30) 70g, acrylic pressure-sensitive adhesive 400g, lauryl lactate 150g, propylene glycol 10g, pH Regulator sodium hydroxide 60g, benzalkonium chloride 10g, total: 1000g.

[0121] Preparation:

[0122] Add donepezil hydrochloride, benzalkonium chloride and polyvinylpyrrolidone (K-30) together to 150g ethanol solution (water: ethanol = 6: 4, volume ratio) after swelling for 4 hours, then add sodium hydroxide solution (hydrogen Add sodium oxide to 50 g of ethanol solution (water: ethanol = 6: 4, volume ratio) to dissolve), mix, adjust the pH to 7.5, and obtain drug reservoir A;

[0123] Add acrylic pressure-sensitive adhesive, propylene glycol and lauryl lactate to the above drug reservoir A, and stir at a speed of 10,000 rpm for 1 hour, mix and disperse, and obtain viscose B containing the drug rese...

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PUM

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Abstract

The invention discloses a transdermal medicament delivery system containing a donepezil compound, a transdermal preparation and a preparation method. The transdermal medicament delivery system comprises the following components in percentage by weight: 0.1 to 50 percent of donepezil or acid radical salt thereof, 1 to 95 percent of skeleton polymer, 0.1 to 60 percent of transdermal penetration enhancer, 0 to 10 percent of cross linker, 0.5 to 60 percent of humectant, 0.02 to 10 percent of bacteriostatic agent, 0.02 to 30 percent of pH regulator and 0 to 90 percent of solvent. The system is used for treating light, medium and severe senile dementia, can maintain long-time stable medicament delivery of at least 3 days, has better performance, is convenient for medicament delivery, and can reduce the administration frequency and increase the compliance of patients; and meanwhile, the transdermal path avoids first-pass effect on gastrointestinal tracts and liver due to oral administration of medicaments, and the system has higher bioavailability and obvious advantages in medicinal application.

Description

technical field [0001] The invention relates to a transdermal drug delivery system containing a donepezil compound, a preparation method and application. Background technique [0002] Alzheimer's disease, also known as Alzheimer's disease (AD), is a primary degenerative encephalopathy that occurs in old age and early old age, and its characteristic pathological changes are cerebral cortex atrophy, accompanied by β-Amyloid deposition, neurofibrillary tangles, loss of number of large memory neurons, and formation of senile plaques. The daily life ability of AD patients is reduced, which brings endless pain and troubles to themselves and the people around them. The average survival period of AD patients is 5.5 years. After cardiovascular disease, cerebrovascular disease and cancer, AD has become the "fourth killer" of the health of the elderly. In the near future, our country will enter an aging society, accompanied by a problem that cannot be ignored - the incidence of AD is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/445A61K47/32A61K47/34A61K47/36A61K47/40A61K47/38A61K9/70A61P25/28A61K47/10
Inventor 罗华菲王浩侯惠民胡婧
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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