尼可地尔在大鼠小肠吸收研究

Intestinal Absorption of Nicorandil in Rats

目的研究尼可地尔在大鼠小肠的吸收特性及吸收动力学。方法采用大鼠在体肠道灌流法,以高效液相色谱(HPLC)法测定灌流液中尼可地尔浓度,考察不同影响因素下尼可地尔的吸收情况并测定吸收动力学参数。结果在不同药物浓度、不同p H值条件下,尼可地尔小肠吸收速率常数间均差异无统计学意义;在肠道各部位的吸收速率按空肠、十二指肠、回肠、结肠顺序下降,分别为(4.69±0.05)×10-2,(3.35±0.04)×10-2,(2.66±0.05)×10-2,(0.89±0.08)×10-2·h-1。结论尼可地尔大鼠在体肠道吸收符合表观一级动力学过程,吸收以被动扩散为主;尼可地尔在整个肠段都有较好吸收,可设计成缓释、控释制剂。

Objective To explore the absorption properties and kinetics of nicorandil from small intestinal segments. Methods The absorption kinetics and permeability of nicorandil under different conditions were investigated by HPLC via the in situ perfusing method in rats. Results There was no significant difference in Ka of nicorandil under different concentrations and different pH.The absorption rate in rats descended in order of jejunum,duodenum,ileum and colon, as （4.69±0.05）×10^-2 ,（3.35 ±0.04） × 10^-2 ,（2.66± 0.05） × 10^-2 and （0.89± 0.08） × 10-2 ·h^-1 . Conclusion The absorption of nicorandil in intestine complies with the passive transport mechanism and first order kinetics.Nicorandil is well absorbed in the whole intestine and can be prepared as delayed release and controlled release forms.