【摘要】 目的 研究阿哌沙班在肾衰大鼠体内的肠吸收特性，并考察P糖蛋白（P-glycoprotein,P-gp）抑制剂对阿哌沙班吸收行为的影响。方法 选择肾衰大鼠在体单向灌流法进行肠吸收实验，建立大鼠阿哌沙班肠灌流液HPLC分析方法，以考察大鼠在体肠吸收影响因素。结果 阿哌沙班在各肠段的吸收速率常数（Ka）存在显著性差异（P<0.05），但表观吸收系数(P_app)未见明显差异（P>0.05）；大鼠回肠段的K_a和P_app值随药物浓度的增加而降低；加入P-gp抑制剂盐酸维拉帕米（0.1 mmol/L）后，阿哌沙班在空肠和回肠段的K_a和P_app值均明显增加。结论 阿哌沙班在各肠段均有吸收；P-gp抑制剂对阿哌沙班在空肠和回肠段的吸收均有明显的促进作用，表明阿哌沙班为P-gp底物，推测其吸收机制为主动转运。更多还原

【Abstract】 Objective To study the intestinal absorption characteristics of apixaban in rats with renal failure, and the effect of P-glycoprotein （P-gp） inhibitors on its absorption behavior. Methods The in vivo absorption experiment was performed in CRF rats by one-way perfusion method and the absorption factors was investigated by establishing the HPLC analysis method.Results The absorption rate constant （K_a） of apixaban in each intestinal segment was significantly different （P<0.05） with no significant difference in apparent absorption coefficient （Papp） （P>0.05）. The K_a and P_app values in the rat ileum decreased with the increasing of drug concentration. After addition of P-gp inhibitor verapamil hydrochloride （0.1 mmol/L）, the K_a and P_app values of apixaban in the jejunum and ileum were significantly increased. Conclusion Apixaban is absorbed in all intestinal segments. P-gp inhibitors can significantly promote the absorption of apixaban in jejunum and ileum, suggesting that apixaban is P-gp substrate and its absorption mechanism is supposed to be active transport.更多还原