人参皂苷Rg3羟丙基-β-环糊精包合物的制备和表征
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摘要
目的考察人参皂苷Rg3羟丙基-β-环糊精包合物的制备工艺及其表征。方法比较研磨法和水溶液搅拌法制备人参皂苷Rg3羟丙基-β-环糊精包合物,以包合率为指标,采用L9(34)正交试验设计优化包合工艺条件,采用薄层色谱法、DSC差热分析、红外光谱法、X-射线衍射法等分析手段对包合物进行表征,测定包合物的体外溶出度。结果选择水溶液搅拌法制备包合物,最佳包合工艺为人参皂苷Rg3与羟丙基-β-环糊精的质量比1∶100,搅拌时间2 h,温度25℃,其包合率为86.11%,通过表征说明包合物已经形成,包合物的溶出速率明显提高。结论人参皂苷Rg3羟丙基-β-环糊精包合物制备工艺稳定可行,溶解性显著提高。
Objective To prepare ginsenoside Rg3 and hydroxypropyl-β-cyclodextrin inclusion complex and to investigate its physical properties.Methods The inclusion complex was prepared by the grinding and aqueous solution-stirring method respectively.Effects of the inclusion conditions were optimized by L9(34)orthogonal test with inclusion rate as index,and the inclusion complex was identified by TLC,DSC,IR and XRD.The dissolution of inclusion complex in vitro was determinated.Results The inclusion complex prepared by the aqueous solution-stirring method had higher inclusion rate.The best inclusion were as followings:ratio of ginsenoside Rg3 and hydroxypropyl-β-cyclodextrin was 1∶100,inclusion time was 2 h,inclusion temperature was 25 ℃.Under these conditions,inclusion rate of ginsenoside Rg3 was 86.11%.All of the characterization methods showed that the inclusion complex had been formed.The dissolution rate of inclusion complex was significantly increased.Conclusions The inclusion technique is stable and feasible,and the solubility of inclusion complex increased obviously.
Objective To prepare ginsenoside Rg3 and hydroxypropyl-β-cyclodextrin inclusion complex and to investigate its physical properties.Methods The inclusion complex was prepared by the grinding and aqueous solution-stirring method respectively.Effects of the inclusion conditions were optimized by L9(34)orthogonal test with inclusion rate as index,and the inclusion complex was identified by TLC,DSC,IR and XRD.The dissolution of inclusion complex in vitro was determinated.Results The inclusion complex prepared by the aqueous solution-stirring method had higher inclusion rate.The best inclusion were as followings:ratio of ginsenoside Rg3 and hydroxypropyl-β-cyclodextrin was 1∶100,inclusion time was 2 h,inclusion temperature was 25 ℃.Under these conditions,inclusion rate of ginsenoside Rg3 was 86.11%.All of the characterization methods showed that the inclusion complex had been formed.The dissolution rate of inclusion complex was significantly increased.Conclusions The inclusion technique is stable and feasible,and the solubility of inclusion complex increased obviously.
引文
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[6]张明明,刘宇,刘墨祥.20(S)-原人参二醇-羟丙基-β-环糊精包合物制备工艺优化研究[J].扬州大学学报(农业与生命科学版),2016,37(1):22-26.
[7]张泰,袁萍,茅仁刚,等.RP-HPLC同时测定西洋参总皂苷转化产物中人参皂苷Rh1、Rg3和Rh2的含量[J].中成药,2010,32(6):1059-1061.
[8]李健莹,栾晓娇,王凯乾,等.人参皂苷Rg3固体分散体的制备及表征[J].中国药学杂志,2015,50(10):872-875.
[9]刘其媛,张振海,金鑫,等.人参皂苷Rg3二元固体分散体的制备及体外特性研究[J].中国中药杂志,2013,38(24):4298-4302.
[2]王鸿彪,林英城.人参皂甙Rg3抗肿瘤作用研究进展[J].医学综述,2009,15(3):323-326.
[3]张翔,叶宝东,陈丹,等.人参皂苷Rg3抗肿瘤机制研究进展[J].中华中医药学刊,2013,2:328-330.
[4]曲晓波,赵雨,宋岩,等.人参皂苷Rg3的拉曼光谱研究[J].光谱学与光谱分析,2008,28(3):569-571.
[5]艾莉,董英杰,张乃先,等.莪术油-羟丙基-β-环糊精包合物的制备与表征[J].沈阳药科大学学报,2007,24(9):528-531.
[6]张明明,刘宇,刘墨祥.20(S)-原人参二醇-羟丙基-β-环糊精包合物制备工艺优化研究[J].扬州大学学报(农业与生命科学版),2016,37(1):22-26.
[7]张泰,袁萍,茅仁刚,等.RP-HPLC同时测定西洋参总皂苷转化产物中人参皂苷Rh1、Rg3和Rh2的含量[J].中成药,2010,32(6):1059-1061.
[8]李健莹,栾晓娇,王凯乾,等.人参皂苷Rg3固体分散体的制备及表征[J].中国药学杂志,2015,50(10):872-875.
[9]刘其媛,张振海,金鑫,等.人参皂苷Rg3二元固体分散体的制备及体外特性研究[J].中国中药杂志,2013,38(24):4298-4302.