目的研究荆芥内酯在大鼠胃肠道的吸收。方法应用大鼠在体胃肠吸收模型,采用酚红标记法校正肠循环液的体积,HPLC法测定不同时间点胃肠循环液中荆芥内酯的质量浓度。结果不同质量浓度(1.84、3.68、7.36μg/mL)的荆芥内酯在大鼠胃部每小时吸收率分别为(19.47±0.69)%、(21.66±1.92)%、(26.51±1.25)%;在大鼠肠道的吸收速率常数(Ka)分别为(0.203±0.007)、(0.159±0.011)、(0.134±0.012)h?1,各组之间差异均显著(P<0.05)。结论荆芥内酯在大鼠胃部的吸收可能为被动转运,在肠道的吸收可能为主动转运。

To study the gastrointestinal absorption kinetics of schizonepetin in rats. Methods The drug concentration by in situ perfusion in rats was determined by HPLC and the volume of perfusion fluid was adjusted by Phenol red labeling. Results The hourly absorption percentages of three different drug concentrations (1.84, 3.68, and 7.36 μg/mL) in stomachs were (19.47 ± 0.69) %,(21.66 ± 1.92) %, and (26.51 ± 1.25) %, respectively. The absorption rate constants (Ka) of three different concentrations in intestine were (0.203 ± 0.007), (0.159 ± 0.011), and (0.134 ± 0.012) h?1, respectively, which had significant differences among them (P<0.05).Conclusion Schizonepetin might be absorbed in stomachs via passive transport mechanism and in intestine via active transport mechanism.

国家科技重大专项课题:创新药物研究开发--候选药物研究(2009ZX09103-339)