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
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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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