23-羟基白桦酸在Caco-2细胞模型中的吸收特性研究  

Intestinal Absorption and Mechanism of 23-Hydroxybetulinic Acid Using Caco-2 Monolayer Model

作　　者：杨敏[1] 王广基[2] 徐宇平[1] 潘栋辉[1] 吴晓兰[2] 黄晨蓉 叶文才[2] 

机构地区：[1]江苏省原子医学研究所,卫生部核医学重点实验室,江苏无锡214063 [2]中国药科大学,南京210009

出　　处：《中国药学杂志》2008年第5期349-352,共4页Chinese Pharmaceutical Journal

基　　金：国家高技术研究发展计划(863计划)资助项目(2003AA2Z347A);江苏省自然基金资助(BK2004025)

摘　　要：目的研究23-羟基白桦酸在Caco-2细胞模型中的吸收特性,为设计合理的给药方式提供依据。方法利用MTT实验筛选出23-羟基白桦酸在Caco-2细胞中的安全浓度,然后用Caco-2细胞单层模型研究23-羟基白桦酸的双向转运,采用同位素示踪法检测药物浓度,计算其表观渗透系数,考察时间、药物浓度对23-羟基白桦酸吸收的影响。结果23-羟基白桦酸在Ca- co-2细胞模型中的转运中对应时间点表观渗透系数值(P_(app))A→B约等于(P_(app))B→A,随时间增加P_(app)逐渐下降,而在所测浓度范围内P_(app)值基本保持恒定。结论23-羟基白桦酸在Caco-2细胞模型中的吸收机制主要是被动转运。OBJECTIVE To investigate the intestinal absorption and the mechanism of 23-hydroxybetulinic acid using Caco-2 monolayer model. METHODS The safety concentration of 23-hydroxybetulinic acid in Caco-2 cell was first selected by using MTT method. Then the Caco-2 cell monolayer model was used to investigate the bi-directional transport of 23-hydroxybetulinic acid and the effect of time and drug concentration on the 23-hydroxybetulinic acid absorption. Drug concentration was measured by radioisotope tracing method and the apparent permeability coefficient （Papp） were calculated. RESULTS In the Caco-2 cell model, the A→B Papp of 23-hydroxybetulinie acid was equal to the B→A Papp and the Papp kept almost constant with the selected concentration investigated. CONCLUSION The 23-hydroxybetolinic acid absorption in Caco-2 cell model is a passive and transeellolar transport. And the absorption of 23-hydroxybetulinic acid in the intestines is quite good.

关 键 词：23-羟基白桦酸 CACO-2细胞模型 被动转运 

分 类 号：R945[医药卫生—微生物与生化药学]