中国中药杂志

2017, v.42(23) 4611-4617

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丹参酮Ⅱ_A/β-环糊精包合物制备工艺优化及体外溶出性能研究
Optimization of preparation procedures of tanshinone-Ⅱ_A/β-cyclodextrin inclusion complex and dissolution study of tanshinone-Ⅱ_A in vitro

吴妮;于洁;张峡;曾敏;张亚军;郑晓晖;
WU Ni;YU Jie;ZHANG Xia;ZENG Min;ZHANG Ya-jun;ZHENG Xiao-hui;The College of Life Sciences,Northwest University;

摘要(Abstract):

采用饱和水溶液法制备丹参酮Ⅱ_A(Tan-Ⅱ_A)与β-环糊精(β-CD)包合物,在单因素试验的基础上,以β-环糊精与丹参酮Ⅱ_A的配比、包合温度和包合时间为自变量,包合物的收率、包封率和总评"归一值"为响应值,使用Box-Benhnken设计效应面法优化丹参酮Ⅱ_A的包合工艺;采用红外光谱法(IR)、核磁共振法(NMR)对包合物进行鉴定。结果表明,丹参酮Ⅱ_A与β-环糊精包合物的最优制备工艺为:丹参酮Ⅱ_A与β-环糊精的配比为1∶7,包合温度为48℃,包合时间为3 h;采用优选的工艺条件制备丹参酮Ⅱ_A与β-环糊精的包封率为84.75%。丹参酮Ⅱ_A与β-环糊精包合物可以明显提高丹参酮Ⅱ_A溶出度。
In this paper,tanshinone-Ⅱ_A(Tan-IIA)/β-cyclodextrin(β-CD) inclusion complexes were prepared by saturated aqueous solution method. Based on the single factor experiment,Box-Benhnken design and response surface method were utilized to optimize the preparation procedures of tanshinone-Ⅱ_A/β-cyclodextrin inclusion complexes. The ratio of β-CD to Tan-Ⅱ_A,experimental temperature and time were defined as independent variables,while the yield of the inclusion complexes,encapsulation efficiency and the generalized " normalized value" were set as the response value. In addition,the inclusion complexes were characterized by infrared spectroscopy(IR) and nuclear magnetic resonance(NMR). The results showed that optimum preparation conditions for Tan-Ⅱ_A/β-CD inclusion complex were as follows: Tan-Ⅱ_A/β-CD ratio of 1: 7,the temperature of 48 ℃ and the time of 3 h. Under the optimized conditions,the encapsulation efficiency of Tan-Ⅱ_A/β-CD inclusion complex was 84. 75%. The Tan-IIAand β-CD inclusion complex can significantly improve the dissolution of Tan-Ⅱ_A.

关键词(KeyWords): 丹参酮ⅡA;β-环糊精;包合工艺;Box-Benhnken设计-效应面法;体外溶出度
Tan-ⅡA;β-CD;inclusion process;box-benhnkendesign and response surface method;dissolution in vitro

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基金项目(Foundation): 陕西省社发攻关项目(2014k14-03-02);; 陕西省重点创新团队计划项目(2013KCT-24)

作者(Author): 吴妮;于洁;张峡;曾敏;张亚军;郑晓晖;
WU Ni;YU Jie;ZHANG Xia;ZENG Min;ZHANG Ya-jun;ZHENG Xiao-hui;The College of Life Sciences,Northwest University;

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