| 在体单向灌流法研究阿哌沙班肾衰大鼠肠吸收特性 |
| 投稿时间：2021-12-06 修订日期：2022-06-29 点此下载全文 |
| 引用本文：张欢,汪丽,张优,谢沛,李娜,丁家荣,王雷.在体单向灌流法研究阿哌沙班肾衰大鼠肠吸收特性[J].药学实践杂志,2022,40(6):515~518,531 |
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| 中文摘要: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（Papp）未见明显差异（P>0.05）；大鼠回肠段的Ka和Papp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Ka和Papp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。 |
| 中文关键词:阿哌沙班 慢性肾衰竭 在体单向肠灌流 肠吸收特征 |
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| Study on intestinal absorption characteristics of apixaban by in vivo one-way perfusion in rats with renal failure |
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| 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 (Ka) 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 Ka and Papp 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 Ka and Papp 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. |
| keywords:apixaban renal failure one-way perfusion intestinal absorption characteristics |
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