正交实验法优化紫草素类脂囊泡的处方工艺

目的优选紫草素类脂囊泡的处方工艺。方法采用薄膜分散法制备紫草素类脂囊泡,以紫草素与司盘60的质量比、司盘60与胆固醇的用量比、磷酸盐缓冲液的用量以及水化时间作为考察因素,将包封率作为考察指标,进行正交实验优化制备工艺。用HPLC法测定包封率,用显微镜观察类脂囊泡的外观形态,并用粒径测定仪测定类脂囊泡的粒径。结果最佳制备工艺为:紫草素与司盘60的比例为1∶20;司盘60与胆固醇的比例为1∶1;磷酸盐缓冲液的用量为15mL;水化时间为30min。所得类脂囊泡的包封率为81.6%;形态为粒径均匀的球形和类球形,粒径为387.6nm,多分散指数PDI为0.476。结论该制备工艺稳定、可行、重复性好,可为工业化生产提供理论依据。

Optimization of formulation and preparation process of shikonin noisomes by or-thogonal design

Objective To optimize the preparation technology of shikonin noisomes.Methods The shikonin noisomes were prepared by thin film hydrolysation method.The preparation was optimized by orthogonal design with encapsulation co-efficiency as index using the ratio of shikonin to Span-60,the ratio of Span-60 to cholesterol,the dosage of phosphate cushion fluid and the time of hydration as factors.The encapsulation efficiency was detected by HPLC.The morphological examination of shikonin noisomes was per-formed using microscopy.The particle size of the noisomse was measured.Results The ideal preparation parameters were as fol-lows:the ratio of shikonin to Span-60 was 1:20,the ratio of Span-60 to cholesterol was 1:1,the dosage of phosphate cushion fluid was 15 mL and the time of hydration was 30 min.The noisomes with spherical or ellipsoidal shape and better stability fea-tured the encapsulation efficiency of 81.6%,the mean particle size of 387.6 nm,and the PDI of 0.476.Conclusion The preparation technology is feasible,stable and reproducible and could be used in industrial production.