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

A technology of levodopa methyl ester and slow-release microspheres, which is applied in the direction of drug combinations, pharmaceutical formulas, and medical preparations containing active ingredients, etc., can solve the problems of inactivation and non-preparation of levodopa methyl ester, and achieve re- good dispersion effect

Inactive Publication Date: 2011-12-07
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

However, there is currently no report on the preparation of levodopa methyl ester and benserazide mixed drug sustained-release microspheres, and a single levodopa methyl ester and benserazide mixed drug sustained-release microspheres are easily degraded by enzymes in the body and inactivated

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] ①Preparation of mixed drug solution of levodopa methyl ester and benserazide

[0029] 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;

[0030] ②Preparation of sustained-release microsphere composition of levodopa methyl ester and benserazide mixed drug

[0031] 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

[0039] ①Preparation of mixed drug solution of levodopa methyl ester and benserazide

[0040]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;

[0041] ②Preparation of sustained-release microsphere composition of levodopa methyl ester and benserazide mixed drug

[0042] 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 fo...

Embodiment 3

[0050] ①Preparation of mixed drug solution of levodopa methyl ester and benserazide

[0051] 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;

[0052] ②Preparation of sustained-release microsphere composition of levodopa methyl ester and benserazide mixed drug

[0053] 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 a levodopa methyl ester and benserazide mixed medicament slow-release microsphere composition. The composition comprises the following components in percentage by weight: 50 to 99 percent of degradable hydrophobic polymer and 1 to 50 percent of levodopa methyl ester and benserazide mixed medicament, wherein the weight ratio of the levodopa methyl ester to the benserazide is 1:1-4:1. The invention also provides a preparation method for the mixed medicament slow-release microsphere composition. The invention overcomes the disadvantage of unavailable effective treatment due to frequent missing of administration caused by the conventional single oral administration scheme and frequent oral administration requirement and provides a W / O / W preparation method. The particle diameter of the composition can be regulated and controlled from 1 to 500mu m according to different requirements without causing environmental pollution; the composition can prevent the influence on the treatment effect of the levodopa methyl ester and benserazide mixed medicament; the solution has the advantages of smooth and round surface, regularity and no adhesion; and the freeze-dried powder of the composition is white, fine, loose, non-collapse and non-adhesive and has high dispersibility.

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 drug sustained-release microsphere composition of mixed levodopa methyl ester and benserazide 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 micros...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P25/16A61K9/16A61K31/216A61K31/165
Inventor 刘振国袁伟恩任甜甜杨新新陈伟
Owner XIN HUA HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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