Formula Optimization of Aprepitant Nanocapsules by Central Composite Design-response Surface Method-ology / 中国药师

ABSTRACT

Objective:To optimize the formula of aprepitant nanocapsules. Methods: The central composite design–response surface methodology was used. The amounts of hydroxg propyl cellulose(HPC-SL) and sodium dodecyl sulfate(SDS) were set as the independent variables;the dissolution of aprepitant capsules at 15min and 30min, and the dissolution after accelerated at 40℃ and 75% RH for 6 months were set as the dependent variables. Quadratic polynomial mathematic models were used to evaluate the relation-ship between the independent and the dependent variables. According to the mathematic models,an effect graph was drawn. The opti-mized formula was chosen from the overlap of the contour graphs of the dependent variables. The similarity of in vitro dissolution curve was evaluated by using f2factor. Results:The correlation coefficient of quadratic polynomial mathematic model and the reliability was high. The measured values of the optimized formula were within the expected ranges. Conclusion: Aprepitant nanocapsules with the optimized formula by central composite design-response surface methodology meet the requirements. The results can provide evidence for the next industrial production.