Donepezils compound long-acting slow-releasing and controlled-releasing composition and preparation method thereof

A technology of donepezil and compounds, which is applied in the field of pharmaceutical preparations to achieve the effects of reducing the number of times of taking medicines, maintaining stable product quality, and mature preparation technology

Inactive Publication Date: 2008-04-30
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although some progress has been made in the research of donepezil preparations, such preparations fail to solve the problems caused by donepezil's need for long-term, daily medication, so a long-acting sustained-release preparation of donepezil is needed clinically and in the market

Method used

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  • Donepezils compound long-acting slow-releasing and controlled-releasing composition and preparation method thereof
  • Donepezils compound long-acting slow-releasing and controlled-releasing composition and preparation method thereof
  • Donepezils compound long-acting slow-releasing and controlled-releasing composition and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0041] Weigh 100 mg of carrier material acrylic resin and dissolve in 2 ml of acetone, drop into 5 ml of donepezil hydrochloride aqueous solution under cooling and magnetic stirring, and add 3 mg of magnesium stearate, slowly drop the mixture into 25 ml of liquid paraffin containing 0.5% Span60 to form The liquid paraffin wraps the acetone emulsifier, and gradually raises the temperature. After 2 to 3 hours, the microparticles are precipitated, washed with n-hexane for several times, and dried under reduced pressure to obtain the acrylic resin long-acting sustained and controlled release composition encapsulating donepezil hydrochloride.

Embodiment 2

[0043] The long-acting sustained and controlled-release composition of donepezil hydrochloride polylactic acid was prepared by emulsification-solvent evaporation method. 100 mg of carrier material polylactic acid was dissolved in 2 ml of chloroform, and 20 mg of donepezil hydrochloride was dispersed in it. Stirring at 800 rpm, slowly added to the dispersion After being emulsified in the medium (1% PVA solution) for 10 minutes, pour into the diffusion medium (0.2% PVA solution) to volatilize the organic solvent, then centrifuge, filter, and dry to obtain the donepezil hydrochloride long-acting sustained and controlled release composition.

Embodiment 3

[0045] Suspend 20mg of donepezil in 10ml of 3% chitosan solution, shake and mix evenly, drop into 30ml of corn oil containing 5% span85 and 0.5% tween 80, emulsify at 200rpm for 15min, add dropwise 2ml of 25% glutaraldehyde to solidify . Then add 40 ml of petroleum ether, stir for 5 minutes and then stand still, discard the upper layer, wash the donepezil long-acting sustained-controlled release composition with isopropanol and petroleum ether successively for 3-5 times, and dry in vacuum to obtain a loose powdery solid long-acting sustained-controlled release composition. release composition. figure 1 The appearance of the long-acting sustained and controlled release composition is round and round, and the average particle size is 10.06 μm.

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Abstract

The invention discloses a long-acting sustained controlled release formulation of donepezil-like composition and a process for preparation. The composition is in the shape of micro-granular. According to the measurement by weight, the invention contains donepezil-like compounds 0.5-5 parts, carrier material of the sustained controlled release formulation 1-500 parts, and further contains other common excipient in pharmacy. The composition is used for anti senile dementia. The frequency of donepezil-like compounds is reduced, and the periodic time of administering medicament is prolonged, the compliance and conformability of the patient are improved, and the bioavailability and the therapeutic index of the donepezil are promoted. Meanwhile the invention discloses a plurality of processes for the preparation of long-acting sustained controlled release formulation of donepezil-like compounds. The process for preparation is flexible. Common processing equipment and commercial scale can be adopted. The production efficiency is high and the quality keeps steady. The invention can be directly or secondly used for making injection or medicament for oral administration.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a pharmaceutical composition of a donepezil compound and a preparation method thereof, more specifically, to a long-acting sustained and controlled release composition containing an anti-senile dementia pharmaceutical active ingredient donepezil compound and its preparation method. Background technique [0002] Donepezil (Donepezil) is a central acetylcholinesterase inhibitor developed by Japan Eisai Pharmaceutical Co., Ltd., with the trade name Aricept, which was approved by the FDA in November 1996 and first listed in the United States in November 1997. Listed in China in October 1999. Currently sold in more than 50 countries in the world. It is a second-generation cholinesterase inhibitor with specific reversibility. When suffering from Alzheimer's disease (AD), the decrease in the concentration of acetylcholine is related to cognitive dysfunction. When acetylcholine...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/445A61P25/28
Inventor 李亚平顾王文陈伶俐
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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