Levodopa methyl ester slow-release microsphere composition and preparation method thereof

A technology of levodopa methyl ester and sustained-release microspheres, which is applied in the direction of drug combinations, pharmaceutical formulas, and medical preparations of non-active ingredients, and can solve the problems of not preparing levodopa methyl ester sustained-release microspheres, etc., to achieve Good redispersibility effect

Inactive Publication Date: 2012-01-18
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

But there is no method report for preparing levodopa methyl ester slow-release microspheres at present

Method used

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  • Levodopa methyl ester slow-release microsphere composition and preparation method thereof
  • Levodopa methyl ester slow-release microsphere composition and preparation method thereof
  • Levodopa methyl ester slow-release microsphere composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] ①Preparation of levodopa methyl ester solution

[0030] a) 100mg levodopa methyl ester is prepared into an aqueous solution with a concentration of 2.5% by weight;

[0031] ②Preparation of levodopa methyl ester sustained-release microsphere composition

[0032] (a) Mix 37.5 mg of polylactic acid (PLA, molecular weight 90,000-140,000) into an organic solution of 15% dichloromethane by weight and 0.5 mL of the above-mentioned ① levodopa methyl ester solution Stir, vortex or sonicate for 1-5 minutes to form a uniform suspension, that is, a water-in-oil (W / O) emulsion; the theoretical percentage of levodopa methyl ester prepared into sustained-release microspheres is 25%.

[0033] (b) adding the emulsion obtained in step (a) to 10 mL of an aqueous solution of 5% sodium chloride and 1% polyethylene glycol (the molecular weight of PVA is 146,000-186,000, alcoholysis degree 98-99%) with a weight percent concentration and Stir, vortex or sonicate for 0.1-5 minutes to form dou...

Embodiment 2

[0041] ①Preparation of levodopa methyl ester solution

[0042] a) 100mg levodopa methyl ester is prepared into an aqueous solution with a concentration of 2.5% by weight;

[0043] ②Preparation of levodopa methyl ester sustained-release microsphere composition

[0044] (a) the polylactic acid (PLA, molecular weight is 90,000-140,000) that weighs 295mg is mixed with the organic solution that is the dichloromethane of 15% concentration by weight and takes 0.2mL above-mentioned ① levodopa methyl ester solution and mixes and Stir, vortex or sonicate for 1-5 minutes to form a uniform suspension, that is, a water-in-oil (W / O) emulsion; the theoretical percentage of levodopa methyl ester to be prepared is 1% sustained-release microspheres.

[0045] (b) adding the emulsion obtained in step (a) to 10 mL of an aqueous solution of 5% sodium chloride and 1% polyethylene glycol (the molecular weight of PVA is 146,000-186,000, alcoholysis degree 98-99%) with a weight percent concentration a...

Embodiment 3

[0053] ①Preparation of levodopa methyl ester solution

[0054] a) 100mg of levodopa methyl ester is prepared to have a concentration of 2.5% by weight;

[0055] ②Preparation of levodopa methyl ester sustained-release microsphere composition

[0056] a) Measure 0.2mL, 0.5mL or 1mL of the levodopa methyl ester solution obtained in ① and weigh 595mg of polylactic acid (PLA molecular weight is 6000), 37.5mg of polylactic acid (PLGA molecular weight is 250,000) or 25mg Polylactic acid (PLGA molecular weight is 500,000) and prepared into organic solutions of dichloromethane with a concentration of 30%, 15% or 5% by weight; 5% and 1 mL of the above-mentioned levodopa methyl ester solutions are mixed one by one correspondingly and stirred, vortexed or sonicated for 1-5 minutes to form a uniform suspension, that is, a water-in-oil (W / O) emulsion; The percentage content of levodopa methyl ester is 1% or 50% slow-release microspheres.

[0057] b) Add the emulsion obtained in step (a) ...

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Abstract

The invention relates to a levodopa methyl ester slow-release microsphere composition, which consists of the following components in percentage by weight: 50 to 99 percent of degradable hydrophobic polymer, and 1 to 50 percent of levodopa methyl ester. The invention also provides a preparation method of the levodopa methyl ester slow-release microsphere composition. The levodopa methyl ester slow-release microsphere composition overcomes the problems that the current oral dosage regimen is single, frequent oral administrations are required, frequent missed administrations are caused to patients of the type, and an effective treatment cannot be achieved; and the preparation method using one type of W / O / W is provided. The grain size of the levodopa methyl ester slow-release microsphere composition can be controlled according to different needs, and the levodopa methyl ester slow-release microsphere composition cannot pollute the environment; and influences on the curative effect of the levodopa methyl ester can be avoided. The grain size can be adjusted and controlled from 1 mu m to 500 mu m according to needs; and freeze-dried powder of the levodopa methyl ester slow-release microsphere composition is white, subtle and loosened, cannot collapse and adhere together, and has high redispersibility. Compared with an oral preparation with the same dosage, the effect of the levodopa methyl ester slow-release microsphere composition is obviously better than that of the oral preparation.

Description

【Technical field】 [0001] The invention relates to a composition in the technical field of pharmaceutical preparations and a preparation method thereof, in particular to a levodopa methyl ester slow-release microsphere composition and a preparation method thereof. 【Background technique】 [0002] In the pharmaceutical industry, from drug discovery to clinical application, the last link is drug preparation. A considerable part of the drugs need long-term frequent administration to be cured; some of them need local administration due to the high toxicity of systemic administration. To achieve these goals, raw materials must be prepared into corresponding dosage forms. For example, drugs that require long-term administration but have a short half-life in the body should be prepared as sustained-release or controlled-release dosage forms; for the treatment of some tumors, some drugs need to be targeted to the disease, such as embolization microsphere preparations that target tumo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/216A61K47/34A61K9/16A61P25/16
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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