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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[0021] Example 1: Take 100 mg of a biodegradable polymer polylactic acid-polyglycolic acid copolymer with a molar ratio of 75:25 and a molecular weight of 50,000, and dissolve it in 3 ml of a methylene chloride solution containing 0.1% lecithin to form an oil phase O ,Add the first water phase W to this oil phase 1 , 0.4ml of amifostine aqueous solution with a concentration of 50mg / ml, emulsify with a phacoemulsifier to obtain W 1 / O emulsion, and then add the obtained emulsion to the second water phase W 2 , 2% polyvinyl alcohol aqueous solution, the ultrasonic emulsifier is again emulsified to obtain W 1 / O / W 2 After the emulsion is formed, magnetic stirring is carried out under ice bath conditions at a stirring speed of 1000 rpm. After stirring and volatilizing for 6 hours, the microspheres are collected by centrifugation at 4°C for 30 min at 6000 rpm and washed with 10 ml of distilled water for 4 times. After pre-freezing, Freeze-drying at -50℃ for 24h. The embedding rate of...
Example Embodiment
[0022] Example 2: Take 100 mg of a biodegradable polymer polylactic acid-polyglycolic acid copolymer with a molar ratio of 75:25 and a molecular weight of 15000, and dissolve it in 3 ml of a methylene chloride solution containing 0.1% lecithin to form an oil phase O. Add the first water phase W 1 , 0.4ml concentration of 50mg / ml amifostine aqueous solution, phacoemulsifier for emulsification, get 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 again emulsified to obtain W 1 / O / W 2 After the emulsion is formed, magnetic stirring is carried out under ice bath conditions at a stirring speed of 1000 rpm. After stirring and volatilizing for 6 hours, the microspheres are collected by centrifugation at 4°C for 30 min at 6000 rpm and washed with 10 ml of distilled water for 4 times. After pre-freezing, Freeze-drying at -50℃ for 24h. The embedding rate of the obtained microspheres is 20%, ...
Example Embodiment
[0023] Example 3: The preparation method is the same as that of 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 in 24h is 68%-80%, and the drug release in vitro can reach 80h.
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