Adefovir dipivoxil liposome injection and its preparing method
A technology of ester lipid and liposome is applied in the field of liposome injection preparation containing adefovir dipivoxil and its preparation, and can solve the problems of instability of adefovir dipivoxil, nephrotoxicity, low bioavailability and the like , to overcome the low bioavailability, reduce toxic and side effects, and improve the efficacy of
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Embodiment 1
[0068] Embodiment 1: the preparation of adefovir dipivoxil liposome injection
[0069] Weigh 3g of adefovir dipivoxil, 20g of soybean lecithin and 7g of cholesterol and put them in a round bottom flask, add an appropriate amount of ethanol to the above mixture to completely dissolve into a clear solution, put it in a constant temperature water bath (75°C) and dry it under reduced pressure to form a film, add Dissolve the film in 1000ml of water for injection, homogenize it with an ultrasonic instrument or a high-pressure homogenizer pump, filter it with a microporous membrane, and pack it in ampoules (or vials), so that each bottle contains 6 mg of adefovir dipivoxil. Sterilize to obtain the liposome for adefovir dipivoxil injection.
Embodiment 2
[0070] Embodiment 2: the preparation of adefovir dipivoxil liposome injection
[0071] Weigh 1g of adefovir dipivoxil, 30g of egg yolk lecithin and 30g of cholesterol and put them in a round bottom flask, add an appropriate amount of chloroform to the above mixture to completely dissolve into a clear solution, put it in a constant temperature water bath (75°C) and dry it under reduced pressure to form a film, add Dissolve the film in 1000ml of water for injection, homogenize it with an ultrasonic instrument or a high-pressure homogenizer pump, filter it with a microporous membrane, and pack it in ampoules (or vials), so that each bottle contains 2 mg of adefovir dipivoxil, Sterilize to obtain the liposome for adefovir dipivoxil injection.
example 3
[0072] Example 3: Preparation of Adefovir dipivoxil liposome injection
[0073] Weigh 3g of adefovir dipivoxil, 30g of egg yolk lecithin, 30g of cholesterol and F 68 Put 27g in a round-bottomed flask, add an appropriate amount of chloroform to the above mixture to completely dissolve into a clear solution, place in a constant temperature water bath (75°C) and dry under reduced pressure to form a film, add 1000ml of water for injection to dissolve the film, and use an ultrasonic machine to ultrasonically pulverize or high-pressure homogenate Homogenize with a pump, then filter with a microporous membrane, pack in ampoules (or vials) so that each bottle contains 2 mg of adefovir dipivoxil, and sterilize to obtain liposomes for injection of adefovir dipivoxil.
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