两种环糊精蓝萼甲素包合物的制备与抗肿瘤作用比较  

Comparation of Inclusion Efficiency and Anti-tumor Effect of Glaucocalyxin A Included by Two Kinds of Cyclodextrin

作　　者：张崇[1] 尚校军[1] 马素英[1] 白素平[1] 

机构地区：[1]新乡医学院药学院,新乡453003

出　　处：《医药导报》2013年第11期1399-1402,共4页Herald of Medicine

基　　金：国家自然科学基金(81072552);新乡医学院第七批省级重点学科开放课题(ZD200903)

摘　　要：目的制备羟丙基-β-环糊精、γ-环糊精蓝萼甲素包合物,比较其体外溶解性能及体内抗肿瘤作用。方法分别用羟丙基-β-环糊精、γ-环糊精制备蓝萼甲素包合物。差示热分析法鉴定,紫外分光光度法测定含量,从相溶解度、溶解度、体外溶出速率以及对小鼠S180移植瘤瘤重的影响方面比较两种包合物。结果蓝萼甲素采用环糊精包合后,相溶解度、溶解度、体外溶出速率均提高,其中γ-环糊精包合作用更好,对小鼠S180移植瘤的抑瘤率43.87%,羟丙基-β-环糊精包合的蓝萼甲素抑瘤率30.66%。结论γ-环糊精包合在改善蓝萼甲素体外溶解性能方面优于羟丙基-β-环糊精,且对S180移植瘤生长的抑制作用更明显。Objective To prepare glaucocalyxin A inclusion complex with two kinds of material and compare their solubility in vitro and anti-tumor effect in vivo. Methods The glaucocalyxin A inclusion complexes were prepared with hydroxypropy-β -cyclodextriu （HP-β-CD） or γ-cyclodextrin （γ-CD）. They were identified by differential thermal analysis （DTA）. UV-spectrophotometry method was applied to determine the contents of glaucocalyxin A. The phase solubility, solubility and dissolution rates of the two complexes and their effects on tumor weight of S^s0 transplantation in mice were compared. Results The phase solubility, solubility and dissolution rates of glaucocalyxin A were enhanced in both kinds of inclusion complex,with γ-CD being a better inclusion material. Tumor inhibition rate against S180 was 43.87% and 30.66% from γ-CD and HP-β-CD included glaucocalyxin A, respectively. Conclusion γ-CD is superior to HP-β-CD for preparation of glaucocalyxin A inclusion complex, demonstrating better solubility, dissolution rate and tumor inhibition properties.

关 键 词：蓝萼甲素 羟丙基-Β-环糊精 Γ-环糊精 

分 类 号：R286[医药卫生—中药学] R965[医药卫生—中医学]