星点设计-效应面法优化柚皮素包合物的制备工艺

Application of the Central Composite Design and Response Surface Methodology to the Preparation Optimization of Naringenin-β-Cyclodextrin Inclusion Complexes

研究星点设计-效应面法优化柚皮素-β-环糊精(NAR-β-CD)包合物的制备工艺。采用搅拌法制备NAR-β-CD包合物,以β-CD与NAR的投料质量比、包合时间、包合温度为自变量,以包封率、包合物得率为因变量,采用星点设计-效应面优化法,对结果进行多元线性回归和二项式拟合,经效应面法预测最佳工艺条件,并作验证试验。并比较NAR-β-CD包合物和NAR的累积溶出率。NAR-β-CD包合物的最佳工艺:β-CD与NAR投料质量比为5∶1,包合时间为1.412 h,包合温度为48.11℃。包合率和包合物得率预测值与理论值的偏差分别为1.43%、1.99%。NAR和NAR-β-CD包合物的累积溶出率分别为37.15%,为83.24%。

The central composite design and response surface methodology were applied to optimize the preparation technology of naringenin-β -cyclodextrin inclusion complexes. The inclusion ratio and the yield of inclusion complexes were studied as independent variables, using several dependent variables such as stirring, the mass ratio of NAR-β -CD, inclusion time, and inclusion temperature. The results were fitted by linear equations and second-order polynomial equation based on the central composite design and response surface method. The optimal inclusion process was predicted according to formulation and further verified by experiments. The cumulative dissolution rates of the NAR-β -CD inclusion complexes and the NAR were comparatively studied. The optimal condition for the preparation of NAR-β -CD inclusion complexes was achieved with a ratio of 5：1 （β -CD： NAR）, inclusion time of 1.412 h,and inclusion temperature at 48.11 ℃ ,where the bias for the prediction value and theoretical value of the inclusion ratio and the yield of inclusion complexes were 1.43% and 1.99%, while the cumulative dissolution rate of NAR and NAR-β -CD inclusion complexes were 37.15% and 83.24%, respectively.