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Sustained release tablet containing donepezil hydrochloride active component as well as preparation method and application thereof

A technology of donepezil hydrochloride and active ingredients, which is applied in the field of sustained-release tablets of the drug donepezil hydrochloride, can solve problems such as side effects and limit clinical efficacy, and achieve the effects of less toxic and side effects, good consistency and low production cost

Inactive Publication Date: 2012-01-11
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, there is a shortcoming in the current immediate-release preparations, because donepezil causes side effects of the cholinergic system within a period of time, such as: nausea, diarrhea, insomnia, vomiting, muscle cramps, etc. This phenomenon that the plasma concentration is too high for a period of time has limited the improvement of the therapeutic dose. On the other hand, because the elimination half-life of donepezil hydrochloride in the blood is 70 hours, adjusting the dose requires a long-term time course, so the lack of common preparations limits the clinical application. curative effect

Method used

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  • Sustained release tablet containing donepezil hydrochloride active component as well as preparation method and application thereof
  • Sustained release tablet containing donepezil hydrochloride active component as well as preparation method and application thereof
  • Sustained release tablet containing donepezil hydrochloride active component as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Regular Tablet Prescription: 100 Tablets

[0049] Donepezil Hydrochloride 1.0g

[0050] Lactose 10.0g

[0051] Starch 5.0g

[0052] Povidone K30 2.0g

[0053] Appropriate amount of water

[0054] Magnesium stearate 0.02g

[0055] Talc powder 0.02g

[0056] Process: pass the main drug and auxiliary materials through a 100-mesh sieve for later use; first weigh lactose, starch, povidone K30 and the main drug donepezil hydrochloride and mix well, then add water-based soft materials, granulate with a 20-mesh sieve, and dry at 55°C About 1 hour, granulate with 18-mesh sieve; finally add talcum powder and magnesium stearate, mix evenly and press into tablets.

Embodiment 2

[0058] Extended-release tablet prescription: 100 tablets

[0059] Donepezil Hydrochloride 0.5g

[0060] Lactose 10.0g

[0061] Pregelatinized starch 3.0g

[0062] Acrylic RS100 4.0g

[0063] 10% povidone K30 aqueous solution appropriate amount

[0064] Magnesium Stearate Appropriate amount

[0065] Process: pass the main drug and other components through a 100-mesh sieve for later use; first weigh the prescription amount of lactose, pregelatinized starch, acrylic resin RS100 and the main drug donepezil hydrochloride and mix well, then add 10% povidone K30 aqueous solution to prepare Soft material, granulated with a 20-mesh sieve, dried at 55°C for about 1 hour, granulated with a 18-mesh sieve; finally, magnesium stearate was added, mixed evenly, and then pressed into tablets.

Embodiment 3

[0067] Extended-release tablet prescription: 100 tablets

[0068] Donepezil Hydrochloride 1.0g

[0069] Lactose 14.0g

[0070] Hypromellose 4000cp 2.0g

[0071] Ethylcellulose 100cp 1.0g

[0072] Sodium Lauryl Sulfate 0.5g

[0073] 2% hypromellose 30% alcohol aqueous solution appropriate amount

[0074] Magnesium Stearate Appropriate amount

[0075] Appropriate amount of talcum powder

[0076] Process: pass the main drug and auxiliary materials through a 100-mesh sieve for later use; first weigh the prescription amount of lactose, hypromellose 4000cp, ethyl cellulose 100cp, sodium lauryl sulfate and the main drug and mix well, then add 2 % Hypromellose (30% alcohol aqueous solution) as soft material, granulated with 20 mesh sieve, dried at 55°C for about 1 hour, granulated with 18 mesh sieve; finally, magnesium stearate and talcum powder were added, mixed evenly, and then compressed into tablets.

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Abstract

The invention discloses a sustained release tablet containing a donepezil hydrochloride serving as an active component. The sustained release tablet provided by the invention comprises the donepezil hydrochloride serving as an active component, a sustained-release material and other auxiliary materials, wherein the weight ratio of the donepezil hydrochloride serving as an active component to the sustained-release material is 1:(0.2-20), preferably 1:(0.5-10) and further preferably 1:(0.7-8). The sustained release tablet containing donepezil hydrochloride prepared by the invention is released steadily, which is favorable for the reduction of the fluctuation of the in-vivo medicament, thus the side effect is reduced, and the sustained release tablet is more suitable for treating patients suffering from Alzheimer-type dementia.

Description

technical field [0001] The invention belongs to the field of drug sustained-release preparations, in particular to a sustained-release tablet of donepezil hydrochloride for treating Alzheimer's disease. Background technique [0002] Senile dementia is a common disease that mainly occurs in the elderly. It is a degenerative disease of the central nervous system mainly characterized by progressive cognitive impairment and memory impairment. The main manifestations are: memory impairment, decreased computing power, visual spatial Disorientation, language impairment, impaired understanding and judgment, emotional and behavioral disturbances. With the advancement of my country's population aging process, the national elderly population is growing at a rate of 3% per year. In 2000, most provinces and cities have entered the aging population structure. For every 10-year-old increase, the prevalence rate will obviously double, 5% for 65 years old, 10% for those over 75 years old, an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/445A61K47/32A61K47/38A61K47/36A61K47/44A61P25/28
Inventor 任晓文徐为人王博连潇嫣李洪起
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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