Donepezil cyclodextrin inclusion compound and oral instant membrane containing same

A technology of cyclodextrin inclusion compound and donepezil, which is applied in the field of medicine, can solve the problems of masking the bitter taste of donepezil, which cannot be realized, and achieve the effect of good taste and fast disintegration and release

Active Publication Date: 2017-11-24
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] Chinese Patent No. 201510443801 describes that donepezil hydrochloride is mixed with adenylic acid, menthol and other auxiliary materials and proce

Method used

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  • Donepezil cyclodextrin inclusion compound and oral instant membrane containing same
  • Donepezil cyclodextrin inclusion compound and oral instant membrane containing same
  • Donepezil cyclodextrin inclusion compound and oral instant membrane containing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Dissolve 0.5g donepezil and 0.984g hydroxypropyl-β-cyclodextrin (molar ratio 1:0.5) in 15mL ethanol, stir at room temperature for 12h, evaporate the solvent, and dry it for later use; add 0.8g hypromellose to 5mL Swell in distilled water under constant temperature magnetic stirring at 65°C, and then dissolve in an ice bath; add 0.54g of donepezil cyclodextrin inclusion compound, 0.32g of glycerin, and 0.1g of CMC-Na to the polymer solution, and stir for 1h Prepare a homogeneous solution, apply it on a glass plate after degassing, dry it at 50°C, and cut it.

Embodiment 2

[0043] Dissolve 0.5g of donepezil and 0.984g of hydroxypropyl-β-cyclodextrin (molar ratio 1:0.5) in 15mL of methanol, stir at room temperature for 12h, evaporate the solvent, and dry it for later use; add 0.8g of polyethylene oxide into 5mL of distilled water , swell under constant temperature magnetic stirring at 65°C, and then dissolve in an ice bath; add 0.54g of donepezil cyclodextrin inclusion compound, 0.32g of glycerin, and 0.1g of CMC-Na to the polymer solution, and stir for 1h to prepare Uniform solution, degassed, coated on a glass plate, dried at 50°C, and cut.

Embodiment 3

[0045] Dissolve 0.5g donepezil and 0.984g hydroxypropyl-β-cyclodextrin (molar ratio 1:0.5) in 15mL water, stir at room temperature for 12h, evaporate the solvent, and dry it for later use; add 0.8g pregelatinized starch into 5mL distilled water , stir to dissolve it; add 0.54g of donepezil cyclodextrin inclusion compound, 0.32g of glycerol, 0.1g of CMC-Na to this polymer solution, stir for 1h to obtain a uniform solution, and coat it on a glass plate after degassing. Dry it at 50°C and cut it.

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Abstract

The invention relates to a taste-masked donepezil cyclodextrin inclusion compound and an oral instant membrane containing the same, belonging to the technical field of medicine. The oral instant membrane comprises the donepezil cyclodextrin inclusion compound, a film-forming material, a plasticizer, a disintegrating agent and other excipients. Specifically, the oral instant membrane is prepared by including donepezil free alkali in cyclodextrin or a derivative thereof, then dissolving the excipients such as the film-forming material in distilled water, adding an appropriate amount of the donepezil cyclodextrin inclusion compound and preparing a homogeneous solution. The donepezil cyclodextrin inclusion compound provided by the invention completely masks the bad taste of donepezil; the oral instant membrane prepared from the donepezil cyclodextrin inclusion compound has good taste, is rapid in drug release and greatly improves patient compliance; moreover, the taste-masked donepezil cyclodextrin inclusion compound can be applied to other oral dosage forms such as tablets and solutions.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to a donepezil cyclodextrin inclusion compound and an oral instant film containing the inclusion compound. Specifically, the present invention relates to an oral fast-dissolving film containing a donepezil cyclodextrin inclusion compound that completely removes bitterness and irritation. Background technique: [0002] Alzheimer's disease, also known as senile dementia, is a chronic progressive disease of the central nervous system. The onset is insidious, the etiology has not yet been elucidated, and the main clinical manifestations are reduced daily life ability, abnormal mental behavior, and cognitive decline, which seriously endanger human health. In my country, the incidence of Alzheimer's disease is increasing year by year. It is known as one of the "four major killers" of the elderly and has brought a heavy burden to society and families. [0003] At present, the drugs appro...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K9/70A61K31/445A61K47/38A61K47/36A61P25/28
CPCA61K9/006A61K9/7007A61K31/445A61K47/36A61K47/38
Inventor 方亮刘婷婷权鹏寸冬梅
Owner SHENYANG PHARMA UNIVERSITY
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