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Microsphere combination medicament containing antiparkinsonism drug and application thereof

A Parkinson's disease and composition technology, which is applied in the field of microsphere compositions, can solve the problems of unstable levodopa nano preparations, easy aggregation of nanoparticles, toxic and side effects, etc., to achieve good medicinal prospects, improve curative effect, reduce The effect of AIM scoring

Inactive Publication Date: 2010-11-10
XIN HUA HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The levodopa nano-preparation is unstable, and the nanoparticles are easy to aggregate, which affects its efficacy, and the excipients used in the levodopa nano-preparation are not pharmaceutical excipients, which have toxic and side effects

Method used

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  • Microsphere combination medicament containing antiparkinsonism drug and application thereof
  • Microsphere combination medicament containing antiparkinsonism drug and application thereof
  • Microsphere combination medicament containing antiparkinsonism drug and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] ①Preparation of mixed drug solution of levodopa methyl ester and benserazide

[0042] a) Mix 100 mg of levodopa methyl ester and benserazide (according to the weight ratio of 1:1) purchased in the market, and prepare the concentration of 2.5% by weight;

[0043] ②Preparation of sustained-release microsphere composition of levodopa methyl ester and benserazide mixed drug

[0044] a) Measure 0.2mL, 0.5mL or 1mL of the mixed drug solution of levodopa methyl ester and benserazide obtained in ①, and weigh 595mg of polyglycolic acid-polylactic acid (PLGA molecular weight is 6000), 37.5mg of Polyglycolic acid-polylactic acid (PLGA molecular weight is 250,000) or 25 mg of polyglycolic acid-polylactic acid (PLGA molecular weight is 500,000) and is prepared into an organic solution of 30%, 15% or 5% by weight concentration of dichloromethane respectively 30% concentration and 0.2mL, 15% and 0.5mL or 5% and 1mL of the above solutions are mixed one by one correspondingly and stirr...

Embodiment 2

[0052] ①Preparation of mixed drug solution of levodopa methyl ester and benserazide

[0053] a) Mixing 100 mg of levodopa methyl ester and benserazide (according to the weight ratio of 2: 1) purchased on the market to prepare a concentration of 2.5% by weight;

[0054] ②Preparation of sustained-release microsphere composition of levodopa methyl ester and benserazide mixed drug

[0055] a) Measure 0.2mL, 0.5mL or 1mL of the mixed drug solution of levodopa methyl ester and benserazide obtained in ① respectively and weigh 595mg of polylactic acid (PLA molecular weight is 6000), 37.5mg of polylactic acid (PLA Molecular weight is 250,000) or polylactic acid (PLA molecular weight is 500,000) of 25mg and is prepared into the organic solution of the methylene chloride of 30%, 15% or 5% by weight percentage concentration respectively; Will use 30% concentration and 0.2mL, 15 % and 0.5mL or 5% and 1mL of the above solutions are mixed one by one and stirred, vortexed or ultrasonically for...

Embodiment 3

[0063] ①Preparation of mixed drug solution of levodopa methyl ester and benserazide

[0064] a) Mix 100 mg of levodopa methyl ester and benserazide (according to the weight ratio of 3:1) purchased in the market, and prepare the concentration of 2.5% by weight;

[0065] ②Preparation of sustained-release microsphere composition of levodopa methyl ester and benserazide mixed drug

[0066] a) Measure 0.2mL, 0.5mL or 1mL of the mixed drug solution of levodopa methyl ester and benserazide obtained in ①, and weigh 595mg of polycaprolactone (PCL molecular weight is 10,000), 37.5mg of polycaprolactone Lactone (PCL molecular weight is 2,500,000) or 25mg of polycaprolactone (PCL molecular weight is 5,000,000) and is prepared into an organic solution of dichloromethane with a concentration of 30%, 15% or 5% by weight; 30% concentration will be used and 0.2mL, 15% and 0.5mL or 5% and 1mL of the above solutions in the order of one-to-one mixing and stirring, vortex or ultrasonic 1-5 minute...

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Abstract

The invention relates to an application of a microsphere composition containing an antiparkinsonism drug to preparation of a medicine for preventing and treating parkinson diseases and complicating diseases of parkinson diseases. The microsphere composition containing the antiparkinsonism drug is selected from benserazide microspheres, L-dopa methyl ester microspheres, the L-dopa methyl ester microspheres and the benserazide microspheres, or L-dopa methyl ester and benserazide mixing drug microspheres. The invention also provides a microsphere combination medicament containing the antiparkinsonism drug. The invention explores novel medical application for the microsphere combination medicament containing the antiparkinsonism drug and develops a novel application field. The microsphere combination medicament containing the antiparkinsonism drug of the invention is safe and nontoxic, has strong pharmacological action and indicates good medicinal prospect.

Description

【Technical field】 [0001] The invention relates to a microsphere composition, in particular to a microsphere combination medicine containing anti-Parkinson's disease medicine and its application. 【Background technique】 [0002] At present, the treatment of Parkinson's disease and symptomatic Parkinson's syndrome mainly includes oral levodopa drugs, which need to be taken three times a day, but it is very inconvenient for these patients because they have problems with movement and memory. It is a very good thing for them if they can achieve the effect of a week or even a month with one medicine. [0003] Chinese patent application number 200910201414.X discloses a selegiline sustained-release microsphere and a preparation method thereof. Chinese patent application number 200910201416.9 discloses a rivastigmine sustained-release microsphere and a preparation method thereof. Chinese patent application number 200410030559.5 discloses levodopa nano-preparation and its preparatio...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/165A61K31/216A61P25/16
Inventor 刘振国袁伟恩杨新新任甜甜陈伟
Owner XIN HUA HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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