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Pharmaceutical composition for parenteral administration, containing donepezil

A technology of donepezil and composition, which is applied in the field of non-oral pharmaceutical compositions containing donepezil, can solve the problems of large drug loss and large dosage, and achieve the effects of improving medication compliance and stabilizing drug release properties for a long time.

Inactive Publication Date: 2016-02-17
DONG KOOK PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

They used a copolymer of lactide and glycolide to prepare microspheres containing donepezil, but the content of donepezil in the microspheres was about 13.2%, and the drug encapsulation rate was only 66%, so there was a lot of drug loss, and The problem that a large amount of administration is required to apply to actual patients

Method used

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  • Pharmaceutical composition for parenteral administration, containing donepezil
  • Pharmaceutical composition for parenteral administration, containing donepezil
  • Pharmaceutical composition for parenteral administration, containing donepezil

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: Preparation of Donepezil Microspheres

[0027] To 1.4g of biocompatible polymer (RESOMERRG858S manufacturer: Boehringer Ingelheim) and 0.6g of donepezilbase (manufacturer: Megafine, India), add 12.6g of dichloride Methane (manufacturer: Merck) was stirred and completely dissolved to obtain a dispersion.

[0028] In the microsphere preparation reactor, add 500 mL of 0.5% polyvinyl alcohol (Mn=30,000~70,000; Sigma) aqueous solution, set it to 10°C, and stir at 3,000 times per minute while using a syringe Slowly add the previously prepared dispersion to prepare microspheres. Then, increase the temperature and volatilize the organic solvent for 2 hours, and then cool for 1 hour to 10°C.

[0029] After washing the prepared microspheres with water for injection several times, they were subjected to wet filtration using sieves of 25 μm and 150 μm, and freeze-dried for 64 hours.

Embodiment 1-1

[0030] Example 1-1: Preparation of microspheres

[0031] A biocompatible polymer (RESOMERRG757S manufacturer: Boehringer Ingelheim) was used, and the rest of the preparation method was implemented in the same way as the method in Example 1, thereby preparing microspheres.

Embodiment 1-2

[0032] Example 1-2: Preparation of microspheres

[0033] In 0.8g of biocompatible polymer (RESOMERRG858S manufacturer: Boehringer Ingelheim) and 1.2g of donepezil base (manufacturer: Megafine, India), 12.6g of dichloromethane (manufacturer: Mo Gram Company) and stirring to make it completely dissolved to obtain a dispersion liquid. The rest of the preparation process was carried out according to the same process as in Example 1 to obtain microspheres.

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Abstract

The present invention relates to a composition for parenteral administration, containing donepezil as an active ingredient, and a preparation method therefor. Donepezil, which has been conventionally used for oral or transdermal administration, is prepared as microparticles comprising a biodegradable and biocompatible polymer and a release controller so as to be provided as a pharmaceutical composition for sustained release parenteral administration, thereby enabling in vivo sustained release continuously for 2-12 weeks or more. Therefore, it is possible to reduce the frequency of administration to a patient and maintain an effective concentration in the blood for a long time.

Description

Technical field [0001] The present invention relates to a parenteral composition containing donepezil as an active ingredient and a preparation method thereof. The purpose of the present invention is to prepare donepezil, which has been used in the form of oral or transdermal administration, to contain biodegradable organisms. Compatible high-molecular polymer and controlled release agent microparticles provide a sustained-release parenteral pharmaceutical composition, which can be continuously released in the body for more than 2-12 weeks to reduce the frequency of administration to patients. And the effect of maintaining effective concentration in the blood for a long time. Background technique [0002] Recently, with the increase of the elderly population, the number of patients with Alzheimer-type dementia has also increased, so patient care has become a serious social problem, and anti-dementia drugs (sntidementia drugs) are rapidly being developed. Donepezil hydrochloride ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/445A61K9/14
CPCA61K9/0073A61K9/1647A61K31/445A61P25/28A61K9/0019A61K9/1682
Inventor 李德根高诚振严信车庚会
Owner DONG KOOK PHARMA CO LTD
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