丹参酮提取物羟丙基-β-环糊精包合物的工艺优化
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摘要
目的优化丹参酮提取物羟丙基-β-环糊精包合物制备工艺。方法在单因素试验的基础上,选择辅料用量、包合温度、超声时间为考察因素,以丹参酮提取物包封率及包合物载药量为综合评价指标,优化丹参酮提取物制备工艺,并采用红外光谱法及指纹图谱技术对包合物进行评价。结果包合物最佳制备工艺为:羟丙基-β-环糊精用量为提取物6倍量,包合温度40℃,超声时间35 min,提取物包封率75.5%,载药量12.1%,包合前后提取物成分基本一致。结论丹参酮提取物羟丙基-β-环糊精包合物包封率高,水溶性好,适合工业生产应用。
Objective To optimize the inclusion process of tanshinone.Methods Based on the results of single factor experiment,the ratio of tanshinone to HP-β-CD,embedded temperature and time were probed.The inclusion process was modified by orthogonal experimental design,and the inclusion complex was identified by IR and HPLC methods.Results The modified inclusion process was as followed: the ratio of tanshinone to HP-β-CD was 1∶6,embedded temperature was 40 ℃ in 35 min.Drug loading and entrapment efficiency were 75.5% and 12.1%,respectively.Conclusion The inclusion process of tanshinone by HP-β-CD is stable,effective,and feasible.
Objective To optimize the inclusion process of tanshinone.Methods Based on the results of single factor experiment,the ratio of tanshinone to HP-β-CD,embedded temperature and time were probed.The inclusion process was modified by orthogonal experimental design,and the inclusion complex was identified by IR and HPLC methods.Results The modified inclusion process was as followed: the ratio of tanshinone to HP-β-CD was 1∶6,embedded temperature was 40 ℃ in 35 min.Drug loading and entrapment efficiency were 75.5% and 12.1%,respectively.Conclusion The inclusion process of tanshinone by HP-β-CD is stable,effective,and feasible.
引文
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[5]潘俊杰,郑琴,杨明.相溶解度法测定不同pH值下丹参酮ⅡA-HP-β-CyD包合稳定常数[J].中成药,2009,31(3):383-386.
[6]罗昕,徐月红,陈宝,等.羟丙基-β-环糊精对隐丹参酮的增溶作用及其包合物的制备[J].中国中药杂志,2005,30(17):1328-1331.
[7]樊丽,闫金红,常永龙,等.环糊精与丹参酮ⅡA包合作用研究[J].化学研究与应用,2009,21(1):31-35.
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[10]李瑞芳,程秀民,毕爱莲.山东不同产地丹参脂溶性成分的高效液相指纹图谱研究[J].中国药业,2010,19(14):21-22.
[11]邓萍,张海东,蒋君好,等.丹参酮分子结构及光谱性质的理论研究[J].计算机与应用化学,2010,27(5):695-698.
[2]Wei Y,Li P,Wang C,et al.Metabolism of tanshinoneⅡA,cryptotanshinone and tanshinoneⅠfrom Radix SalviaMiltiorrhiza in zebrafish[J].Molecules,2012,17(7):8617-8632.
[3]Zhou X,Wang Y,Or PM,et al.Molecular docking and en-zyme kinetic studies of dihydrotanshinone on metabolism of amodel CYP2D6 probe substrate in human liver microsomes[J].Phytomedicine.2012,19(7):648-657.
[4]刘梅,夏鑫华.丹参酮ⅡA化学稳定性研究[J].中药材,2010,33(4):606-609.
[5]潘俊杰,郑琴,杨明.相溶解度法测定不同pH值下丹参酮ⅡA-HP-β-CyD包合稳定常数[J].中成药,2009,31(3):383-386.
[6]罗昕,徐月红,陈宝,等.羟丙基-β-环糊精对隐丹参酮的增溶作用及其包合物的制备[J].中国中药杂志,2005,30(17):1328-1331.
[7]樊丽,闫金红,常永龙,等.环糊精与丹参酮ⅡA包合作用研究[J].化学研究与应用,2009,21(1):31-35.
[8]国家药典委员会.中华人民共和国药典[S].一部.北京:中国医药科技出版社,2010:71.
[9]国家药典委员会.中华人民共和国药典[S].一部.北京:中国医药科技出版社,2010:375.
[10]李瑞芳,程秀民,毕爱莲.山东不同产地丹参脂溶性成分的高效液相指纹图谱研究[J].中国药业,2010,19(14):21-22.
[11]邓萍,张海东,蒋君好,等.丹参酮分子结构及光谱性质的理论研究[J].计算机与应用化学,2010,27(5):695-698.