Preparation and Quality Study of Aripiprazole Long Acting Microcrystalline Injection
Objective:The quality attributes of aripiprazole monohydrate(ALM)from different sources are compared,and the long-acting microcrystalline injection of aripiprazole is prepared using wet grinding technology to investigate its in-vitro release characteristics and stability.Methods:By searching for formulation information of the reference listed drug(RLD),ALM is selected as the active pharmaceutical ingredient(API),carboxymethyl cellulose sodium(CMC-Na)as the stabilizer,and D-mannitol as the freeze-dried protective agent,and the process parameters of medium grinding is optimized.Results:After optimization,it is determined that Supplier 3 is selected as the API vendor,CMC-Na of Model A as the suspension agent and D-mannitol of delta crystal form as the freeze-dried protective agent.In formulation process,a suspension with an average particle size of 2.5 µm and a span of 1.9 to 2.1 can be obtained after wet ground at 2 000 r/min for 20 minutes using 0.3 mm zirconia beads with 70%filled.Conclusion:There are slight differences in the quality of ALM from different sources;the long-acting microcrystalline injection of aripiprazole can release up to 90%in 0.25%sodium lauryl sulfate solution within 480 minutes,exhibiting a similar in vitro release behavior with the reference formulation,and showing good stability after stored at 45℃RH and 75%RH for 6 months.
wet medium grindingmicrocrystalaripiprazolevacuum freeze-drying
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