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Aclacinomycin nanometer grain and preparation method thereof

A technology of aclarithromycin and nanoparticles, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, organic active ingredients, etc., and can solve problems such as high selectivity, secondary antigen-antibody reactions, and low drug loading , to increase the amount of drugs, eliminate toxicity and side effects, and improve the effect of treatment

Inactive Publication Date: 2012-09-12
THE FIRST AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIVERSITY OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Antibody-mediated drug targeting, high selectivity, good directional behavior, but low drug loading, secondary antigen-antibody reactions, etc.

Method used

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  • Aclacinomycin nanometer grain and preparation method thereof
  • Aclacinomycin nanometer grain and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] The preparation method of the aclarithromycin nanoparticles of the present embodiment comprises the following steps:

[0022] a. Take 1 volume part of organic solvent as the oil phase solution solvent, and dissolve 10% aclarmycin A or aclarmycin B in the organic solvent according to the total volume percentage of the oil phase; The content is 2.5% of phospholipids and bile salts, and the ratio of phospholipids to bile salts is 8:2. The phospholipids are dissolved in organic solvents to form an oil phase solution; wherein, the organic solvents are low-boiling organic solvents, such as methylene chloride, trichloro Methane, ethyl acetate, benzene or toluene; The present embodiment adopts dichloromethane, certainly adopt other low-boiling point and the organic solvent that can not cause damage to aclarithromycin can also achieve the purpose of the invention; Low-boiling point organic solvent is easy to follow-up process Evaporation in medium is conducive to the preparation...

Embodiment 2

[0028] The preparation method of the aclarithromycin nanoparticles of the present embodiment comprises the following steps:

[0029] a. Get 4 parts by volume of organic solvent as the oil phase solution solvent, and dissolve 2% aclarmycin A or aclarithromycin B in the organic solvent according to the total volume percentage of the oil phase; The content is 1.25% of phospholipid and bile salt, the ratio of phospholipid to bile salt is 1:4, and the phospholipid is dissolved in an organic solvent to form an oil phase solution; wherein, the organic solvent is a low-boiling organic solvent, such as dichloromethane, trichloro Methane, ethyl acetate, benzene or toluene; The present embodiment adopts chloroform, and of course adopts other low boiling point organic solvents that will not cause damage to aclarithromycin; the purpose of the invention can also be achieved; the low boiling point organic solvent is easy to follow-up process Evaporation in medium is conducive to the preparat...

Embodiment 3

[0034] The preparation method of the aclarithromycin nanoparticles of the present embodiment comprises the following steps:

[0035] a. Get 4 parts by volume of organic solvent as the oil phase solution solvent, and dissolve 14% aclarmycin A or aclarmycin B in the organic solvent according to the total volume percentage of the oil phase; The content is 6.25% of phospholipids and bile salts, and the ratio of phospholipids to bile salts is 1:4. The phospholipids are dissolved in an organic solvent to form an oil phase solution; wherein, the organic solvent is a low-boiling organic solvent, such as methylene chloride, trichloro Methane, ethyl acetate, benzene or toluene; The present embodiment adopts ethyl acetate, certainly adopt other low-boiling point and the organic solvent that can not cause damage to aclarithromycin can also achieve the purpose of the invention; Low-boiling point organic solvent is easy to follow-up process Evaporation in medium is conducive to the preparat...

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PUM

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Abstract

The invention discloses an aclacinomycin nanometer grain and a preparation method thereof. The aclacinomycin nanometer grain is not attached to a carrier material and is directly applied to ensure that the drug dosage can be increased, the toxicity and the side effect which are caused by the carrier can be eliminated and the treatment effect can be improved; in the preparation method, a low-boiling-point organic solvent is combined with an emulsification technology and process to directly prepare the aclacinomycin (comprising aclacinomycin A and aclacinomycin B) nanometer grain without the carrier material; and the aclacinomycin nanometer grain prepared by utilizing the preparation method provided by the invention has a spherical appearance and a rounding and smooth surface, and the grainsize is in a range of 10-1000nm.

Description

technical field [0001] The invention relates to medicine and a preparation method thereof, in particular to a clarithromycin nanoparticle and a preparation method thereof. Background technique [0002] The effect of drug therapy depends on the concentration of the drug at the site of action or the effector tissue or organ. Targeted drug therapy is a field that has developed rapidly in the past two decades and has been studied in many fields. The purpose is to increase the drug concentration at the site of action or effect tissue and organ through targeted delivery of drugs, and reduce the drug concentration in other tissues and organs of the body, thereby improving drug treatment effect , to reduce toxic and side effects, there are two main forms: one is antibody-mediated drug targeting, the drug is combined with the antibody through chemical cross-linking, and the drug is actively guided to the receptor and other effect sites through the antigen-antibody binding reaction in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/704A61P35/00
Inventor 王章阳孟晓红刘松青夏培元陈剑鸿刘耀赵映兰
Owner THE FIRST AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIVERSITY OF PLA
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