羟丙基-β-环糊精包合物中丹参脂溶性成分吸收机理的研究  

Studies on Absorptive Mechanism of Lipophilic Components of Danshen from its Hydroxypropyl-β-Cyclodextrin Inclusion Complex

作　　者：王凌[1] 蒋学华[1] 周静[1] 杨俊毅[1] 

机构地区：[1]四川大学华西药学院,成都610041

出　　处：《生物医学工程学杂志》2006年第3期592-596,共5页Journal of Biomedical Engineering

基　　金：国家自然科学基金资助项目(30271614)

摘　　要：以丹参酮IIA为目标成分,建立了用高效液相色谱仪测定丹参脂溶性成分在大鼠肠循环液中浓度的方法。通过大鼠在体肠循环实验,分别用米氏方程及F ick's扩散公式对结果进行拟合,考察丹参醇提取物在体内吸收的限速过程。结果表明丹参醇提取物在体内吸收的限速过程为溶出过程,并根据此结论指导剂型的设计。制备得到了丹参醇提取物的羟丙基-β-环糊精包合物,并研究其吸收机理。给予三种不同剂量的丹参酮IIA包合物肠循环液后,吸收速率常数K a之间无显著差异。提示包合物中丹参酮IIA吸收的转运机制是被动转运。Taking Tanshinon ⅡA as the target and using reversed phase high performance liquid chromatography,we have developed a rapid and sensitive assay for lipophilic components of Danshen （LCD） in perfusate. The model of intestinal absorption was used to determine the concentration of Tanshinon ⅡA in rats as an in situ model. The change of concentration of Tanshinon ⅡA was separately calculated according to Michaelis Menten and the Fick＇s equation to investigate the absorptive limit step of the LCD. It was concluded that the limit step to absorption of LCD was at the dissolution, by assessing the fitting index or correlative index. On the basis of the conclusion, the experiment was designed to prepare the inclusive complex of the LCD with hydroxypropyl-β- cyclodextrin （HP-β-CD）and to study its absorptive mechanism. With the increase of dosage of complex, its absorption did not show saturated phenomenon in gastro-intestinal tract in rats and the constant Ka did not show significant difference, suggesting that the transport of mechanism in vivo is similar to passive transport.

关 键 词：丹参酮Ⅱ A 包合物 羟丙基-Β-环糊精 在体肠吸收 

分 类 号：R283[医药卫生—中药学]