[关键词]
[摘要]
目的 优化丹参二萜醌(diterpenoid tanshinone,DT)羟丙基-β-环糊精(hydroxypropyl-β-cyclodextrin,HP-β-CD)包合物(inclusion complex,IC)(DT&HP-β-CD@IC)制备工艺。方法 在单因素试验的基础上,选择DT与HP-β-CD的配比、包合温度、包合时间为考察因素,以DT包封率及包合物载药量为综合评价指标,利用Box-Behnken响应面优化DT&HP-β-CD@IC制备工艺,并采用红外光谱法、紫外光谱法、薄层色谱法及扫描电子显微镜法对DT&HP-β-CD@IC进行评价。结果 DT&HP-β-CD@IC最佳制备工艺为HP-β-CD质量浓度0.1 g/mL,药物与载体材料配比1∶3,包合时间2 h,包合温度40 ℃。DT&HP-β-CD@IC的包封率达68.78%,载药量达5.44%。紫外、红外光谱和薄层色谱等结果表明DT&HP-β-CD@IC的形成。结论 DT&HP-β-CD@IC载药量较高,溶解性有一定的提高。
[Key word]
[Abstract]
Objective To optimize the preparation process of diterpenoid tanshinone (DT) hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex (IC) (DT&HP-β-CD@IC). Methods Based on the single factor test, the ratio of DT and HP-β-CD, the inclusion temperature, and the inclusion time were selected as the investigating factors, the encapsulation efficiency and drug-loading of the inclusion complex were used as the evaluation index. The Box-Behnken response surface was used to optimize the preparation process of the DT&HP-β-CD@IC, and the inclusion complex was evaluated by infrared spectroscopy, ultraviolet spectroscopy, thin layer chromatography and scanning electron microscopy. Results The optimal preparation process of the inclusion complex was as follows: HP-β-CD concentration was 0.1 g/mL, the ratio of drug to carrier material was 1:3, the inclusion time was 2 h, and the inclusion temperature was 40 ℃. The encapsulation rate of DT&HP-β-CD@IC was 68.78%, and the drug loading was 5.44%. The results of ultraviolet, infrared spectroscopy and thin-layer chromatography indicated the formation of inclusion complex. Conclusion DT&HP-β-CD@IC has a high encapsulation efficiency and a certain improvement in solubility.
[中图分类号]
R283.6
[基金项目]
浙江省科技计划项目省级重点研发计划(2019C03072);浙江省中医药科技计划项目(2023ZR081)