星点设计-响应面法优化千斤拔黄酮-β-环糊精包合工艺

陈帅; 王慧竹; 姜昆; 钟方丽

doi:10.13386/j.issn1002-0306.2016.02.048

星点设计-响应面法优化千斤拔黄酮-β-环糊精包合工艺

1. 吉林化工学院化学与制药工程学院
2. 沈阳药科大学药学院

基金项目:

吉林省教育厅科研基金资助项目(吉教科合字[2013]第470号)；吉林化工学院科技项目(吉化院合字[2012]第051号)；

详细信息

作者简介:
陈帅(1982-),男,硕士,讲师,研究方向:中药新剂型与新技术,E-mail:chenshuai2011@163.com。;

钟方丽(1970-),女,博士,教授,研究方向:天然产物化学开发及应用,E-mail:fanglizhong@sina.com。;

中图分类号: TQ461
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出版历程
- 收稿日期: 2015-08-02

Optimization of the inclusion process of flemingia flavonoids with β-cyclodextrin by central composite design and response surface methodology

School of Chemistry and Pharmaceutical Engineering,Jilin Institute of Chemical Technology
College of Pharmacy,Shenyang Pharmaceutical University

摘要

摘要: 本研究以优化千斤拔黄酮-β-环糊精包合工艺,并验证包合物的增溶作用为目的。在预实验基础上,利用红外分光光度法验证了千斤拔黄酮-β-环糊精包合物的形成,然后采用饱和水溶液法,在单因素实验基础上,以包合物得率和包合率总评归一值为考察指标,采用响应面法优化千斤拔黄酮-β-环糊精包合物的制备工艺。预实验结果表明千斤拔黄酮-β-环糊精包合物已经形成,响应面实验显示包合物的最佳制备工艺条件为:β环糊精与千斤拔黄酮投料比（质量比）5.5∶1、包合温度43℃、包合时间3.8 h,在此最佳工艺条件下,千斤拔黄酮-β-环糊精包合物的包合率为44.68%,包合物得率为73.12%,溶解度测定结果表明将千斤拔黄酮利用β环糊精包合后,可使千斤拔黄酮在水中溶解度由（22.86±0.62）mg提高到（106.58±0.95）mg。千斤拔黄酮与β环糊精可形成稳定的包合物,包合物的形成可使千斤拔黄酮在水中的溶解度显著提高,为千斤拔黄酮口服制剂的开发提供了理论依据。
- 千斤拔黄酮 /
- β环糊精 /
- 包合工艺 /
- 星点设计 /
- 响应面法
Abstract: The aim of the experiment was to optimize the inclusion process of Flemingia flavonoids-β-cyclodextrin(TFF-β-CD) inclusion compound and identify its solubilization effect. On the basis of the pre-experiment,the formation of the inclusion compound was confirmed by infrared spectrophotometry. Using saturated aqueous solution method and the single factor test, response surface experiment was carried out to optimize the preparation process of TFF-β-CD inclusion compound with overall desirability of inclusion rate and yield as appraisement criteria. The result of pre- experiment showed that the TFF- β- CD inclusion compound had formed while the result of response surface methodology experiment showed that the optimum preparation process of TFF-β-CD inclusion compound was as follows:the feed ratio of β-cyclodextrin and TFF(mass ratio)5.5∶1,inclusion temperature 43 ℃,inclusion time 3.8 h and under the optimum conditions,the inclusion rate and the yield of the inclusion compound was 44.68% and 73.12% respectively. The solubility test showed that the solubility of TFF increased from(22.86±0.62) mg to(106.58±0.95) mg in water because of the preparation of TFF-β-CD inclusion compound. The TFF and β-CD could form stable inclusion complexes,the formation of which could increase the solubility of TFF in water significantly. Moreover the results of experiment provided a theoretical basis for the development of the oral preparation of TFF.
- Philippine flemingia /
- β-cyclodextrin /
- inclusion technology /
- central composite design /
- response surface methodology

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