Method for preparing amifostine microspheres

A technology of amifostine and microspheres, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, and pharmaceutical formulas, etc., can solve the problems of short action time and the like

Inactive Publication Date: 2010-02-03
NORTHWESTERN POLYTECHNICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to overcome the problem of short drug action time of amifostine freeze-dried powder in the prior art, the present invention provides a preparation method of amifostine microspheres. Amifostine is embedded in biodegradable polymer materials to prepare ammonia Fostin microspheres, which can prolong the drug action time

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: get molar ratio and be 75: 25, molecular weight is 50000 biodegradable polymer polylactic acid-polyglycolic acid copolymer 100mg, be dissolved in the methylene chloride solution that contains 0.1% lecithin in 3ml, form oily phase. , add the first water phase W to this oil phase 1 , 0.4ml concentration is the amifostine aqueous solution of 50mg / ml, carries out emulsification with ultrasonic emulsifier, obtains W 1 / O emulsion, and then add the resulting emulsion to the second aqueous phase W 2 , 2% polyvinyl alcohol aqueous solution, the ultrasonic emulsifier is emulsified again, and W 1 / O / W 2 After forming the emulsion, magnetic stirring was carried out under ice bath conditions at a stirring speed of 1000rpm. After stirring and volatilization for 6h, centrifuge at 4°C for 30min at a speed of 6000rpm to collect the microspheres, repeat washing 4 times with 10ml distilled water, and then pre-freeze. Freeze-dry at -50°C for 24 hours. The encapsulation r...

Embodiment 2

[0022] Embodiment 2: get molar ratio and be 75: 25, biodegradable polymer polylactic acid-polyglycolic acid copolymer 100mg of molecular weight 15000, be dissolved in the dichloromethane solution that contains 0.1% lecithin in 3ml, form oil phase O, Add the first aqueous phase W 1 , 0.4ml concentration is 50mg / ml amifostine aqueous solution, emulsifies with ultrasonic emulsifier, gets W 1 / O emulsion, the obtained emulsion is added to the second water phase W 2 , 2% polyvinyl alcohol aqueous solution, the ultrasonic emulsifier is emulsified again, and W 1 / O / W 2 After forming the emulsion, magnetic stirring was carried out under ice bath conditions at a stirring speed of 1000rpm. After stirring and volatilization for 6h, centrifuge at 4°C for 30min at a speed of 6000rpm to collect the microspheres, repeat washing 4 times with 10ml distilled water, and then pre-freeze. Freeze-dry at -50°C for 24 hours. The embedding rate of the obtained microspheres is 20%, the diameter of ...

Embodiment 3

[0023] Embodiment 3: The preparation method is the same as in Example 1, wherein the biodegradable polymer is a polylactic acid-polyglycolic acid copolymer with a molar ratio of 50:50 and a molecular weight of 15000. After testing, the embedding rate of the microspheres is 25%. The spherical particle size is 400-800nm, the cumulative release is 68%-80% in 24 hours, and the drug release in vitro reaches 80 hours.

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Abstract

The invention discloses a method for preparing amifostine microspheres, comprising the following steps: adopting an emulsification-solvent evaporation method to dissolve biodegradable polymers into organic solvents, adding surfactant, mixing with amifostine aqueous solution, emulsifying the mixture by an ultrasonic emulsifier, dispersing emulsion into polyvinyl alcohol aqueous solution to undergofurther ultrasonic emulsification to form w / o / w type emulsion, carrying out magnetic stirring on the w / o / w type emulsion under low temperature to volatilize the organic solvents, then carrying out centrifuging, washing and freeze drying to obtain the amifostine microspheres. By using the method of the invention, the organic solvent is low in usage amount, the preparation time is short, the grain sizes of the microspheres are controlled between 400nm and 900nm and the in-vitro release time of the microspheres lasts as long as 75-100h.

Description

technical field [0001] The invention relates to a preparation method of microspheres, in particular to a preparation method of amifostine microspheres. Background technique [0002] Amifostine (WR-2721, amifostine) was approved by the US FDA in 1999 for anti-nephrotoxicity of chemotherapy drugs and for reducing xerostomia caused by radiotherapy in tumor patients. It is also a good radiation protection and cell protection agent. There are significant effects in the injury of tumor chemotherapy, but there are inherent deficiencies in its clinical use. Firstly, the plasma clearing speed is very fast, less than 10% of the drug remains in the blood 6 minutes after intravenous injection, and the drug has a short duration of action; secondly, oral administration is ineffective and has side effects such as nausea, vomiting, and acute hypotension. [0003] The document "Chinese Patent Publication No. CN1291475" discloses a freeze-dried amifostine powder preparation and its preparati...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/661A61K47/34A61K47/36A61K47/42A61P1/02A61P39/00
Inventor 卢婷利孙伟光于洋陈涛
Owner NORTHWESTERN POLYTECHNICAL UNIV
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