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

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.

Formula Optimization of Regorafenib Solid Dispersion by Orthogonal Test / 中国药师

Objective:To optimize the formula of regorafenib solid dispersion .Methods: On the basis of preliminary studies on the carrier and drug/carrier ratio, an orthogonal test was used to study the formula of regorafenib solid dispersion .The orthogonal table of L9 (34 ) was designed to study the drug/carrier ratio, ultrasound time and bath temperature .Results: Regorafenib solid dispersion was prepared by a solvent method with polyvinylpyrrolidone K 30 as the carrier.The drug/carrier ratio was 1 ∶7, the ultrasound time was 4min, and the bath temperature was 30℃.Regorafenib solid dispersion showed good stability confirmed by differential scanning calorimetry and X-ray diffraction .The dissolution in 30 min reached above 90 %.Conclusion: The preparation process is stable and reproducible , which can be used to prepare regorafenib solid dispersion .