盐酸巴马汀在caco-2细胞中的吸收机制研究 - 中国实验方剂学杂志.doc

盐酸巴马汀在Caco-2细胞中的吸收机制研究 廖琼峰1 谭晓婧 1,2 毕开顺2 张蕾1 谢智勇3* （1. 广州中医药大学中药分析教研室，广东广州510006；2. 沈阳药科大学药学院，辽宁沈阳110016；3.中山大学药学院，广东广州510080） 摘要：目的：研究盐酸巴马汀在Caco-2细胞模型中的吸收机制。方法：用Caco-2细胞单层模型研究盐酸巴马汀的双向转运，并考察时间、药物浓度、抑制剂、pH值及温度对盐酸巴马汀吸收的影响。用高效液相色谱法检测药物浓度，计算其表观渗透系数。结果：盐酸巴马汀在Caco-2细胞模型中，从单层细胞层顶端到基底端的转运大于基底端到顶端的转运，随时间和浓度的增加，药物吸收呈饱和趋势，且P-糖蛋白（P-glycoprotein, P-gp）抑制剂维拉帕米、pH值和温度对它的转运有影响。结论：盐酸巴马汀在Caco-2细胞模型中的吸收主要是由载体介导的主动转运，且该主动转运的载体位于Caco-2细胞单层的顶端。 关键词：盐酸巴马汀；Caco-2细胞模型；主动转运 中图分类号： 文献标识： 文章编号： Absorption mechanism of palmatine chloride across Caco-2 cell monolayer mode LIAO Qiong-feng1 TAN Xiao-jing 1,2 BI Kai-shun2 ZHANG Lei1 XIE Zhi-yong3* (1. Department of Pharmaceutical Analysis, Guangzhou University of Chinese Medicine, 510006, China; 2. School of pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China; 3. School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510080,China) Abstract:Objective: to investigate the absorption mechanism of palmatine chloride by using Caco-2 monolayer mode1.Methods: A Caco-2 cell monolayer model was used to investigate the bi-directional transport of palmatine chloride. The effect of time, drug concentration, temperature, pH and inhibitors on the absorption of palmatine chloride was studied. Apparent permeability coefficient (Papp) of palmatine was calculated based on quantitation by HPLC. Results: Directional flux studies with palmatine chloride suggested transport with the permeability in the apical to basolateral direction higher than that in the basolateral to apical direction. Transport of palmatine chloride could be of saturation with time and concentration, and it was also effected by P-glycoprotein inhibitor, pH and temperature. Conclusion:The absorption of palmatine chloride in Caco-2 cell model was an active transportation mediated by transporter, which mainly located in the apical side ofCaco-2 cell monolayer. Key words: palmatine chloride; Caco-2 cell model; active transport 盐酸