莱菔子水提液中芥子碱硫氰酸盐在大鼠小肠的吸收特性研究  

Studies on Intestinal Absorption of Sinapine Cyanide Sulfonate of Semen Raphani Water Extract in Rats

作　　者：朱立俏[1] 盛华刚[1] 周洪雷[1] 

机构地区：[1]山东中医药大学,山东济南250355

出　　处：《中药新药与临床药理》2014年第4期459-462,共4页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：山东省自然科学基金项目(ZR2010HM017);山东省高等学校科技计划项目(J105LL05);山东中医药大学校级课题(ZYDXY1332)

摘　　要：目的研究莱菔子水提液中芥子碱硫氰酸盐在大鼠小肠的吸收特性。方法采用大鼠在体单向肠灌流模型,用HPLC法对芥子碱硫氰酸盐质量浓度进行分析,计算其吸收速率常数和表观吸收系数,分别研究药物质量浓度和P-糖蛋白(P-gp)抑制剂对芥子碱硫氰酸盐吸收的影响。结果芥子碱硫氰酸盐在大鼠小肠的吸收速率常数(Ka)和表观吸收系数(Papp)随浓度增加先增加后减小,且芥子碱硫氰酸盐的表观吸收速率小于1.8伊10-4cm·min-1,P-gp抑制剂对芥子碱硫氰酸盐的吸收具有显著影响(P<0.01)。结论芥子碱硫氰酸盐在大鼠小肠中的吸收机制可能为主动转运或易化扩散,且其在小肠中的吸收较差,芥子碱硫氰酸盐为P-gp底物。Objective To investigate the intestinal absorption of sinapine cyanide sulfonate of Semen Raphani water extract in rats. Methods The concentration of sinapine cyanide sulfonate was analyzed by HPLC and by using rat in-vivo single-pass intestinal perfusion model. The effects of drug concentration and P-glycoprotein （P-gp） inhibitors on the intestinal absorption of sinapine cyanide sulfonate were evaluated by calculating absorption rate constant （Ka） and apparent absorption coefficient （Papp）. Results The absorption rate constant （Ka）and the apparent absorption coefficient （Papp） of sinapine cyanide sulfonate were increased firstly and then decreased with the increase of concentration. The apparent absorption coefficient （Papp） was lower than 1.8×10^-4 cm·min-1. P-gp inhibitors had significant effect on the absorption of sinapine cyanide sulfonate（P 〈 0.01 ）. Conclusion The absorption mechanism of sinapine cyanide sulfonate in rat small intestine may be in active transport or facilitated diffusion. Sinapine cyanide sulfonate has poor intestinal absorption, and sinapine cyanide sulfonate is proved to be a substrate of P-gp.

关 键 词：莱菔子 芥子碱硫氰酸盐 在体单向肠灌流模型 肠吸收 

分 类 号：R285.5[医药卫生—中药学]