反式曲马朵在大鼠小肠中吸收的立体选择性

目的研究反式曲马朵(Trans T)在大鼠小肠中吸收的立体选择性。方法高效毛细管电泳法测定小肠分段灌流液中Trans T对映体的浓度。结果Trans T对映体在小肠不同部位的吸收分数基本一致;在低浓度时(+)-Trans T的吸收分数明显低于(-)-Trans T;在高浓度时Trans T对映体的吸收分数降低,(+)-Trans T与(-)-Trans T的吸收分数无明显差别。结论Trans T在大鼠小肠的不同部位均能被吸收,具立体选择性,以(-)-Trans T占优。

Stereoselectivity in absorption of trans tramadol in rat intestine

AIM: To investigate the stereoselectivity in absorption of trans tramadol (trans T) in rat intestine. METHODS: The duodenum, jejunum and ileum were separately perfusated in situ with trans T dissolved in Krebs-Ringer buffer. Trans T enantiomers in the perfusate were analyzed with a high performance capillary electrophoresis (HPCE) method. RESULTS: The absorbed fractions of trans T enantiomers were similar among the different segments of the rat intestine. The absorbed fraction of (+)-trans T was lower than that of (-)-trans T when the concentration of trans T was not higher than 40 mumol.L-1. As the concentration of trans T increased, the absorbed fractions of trans T enantiomers were reduced and the difference in absorbed fractions between trans T enantiomers became not significant. CONCLUSION: Trans T enantiomers can be absorbed in different parts of the rat intestine. The intestinal absorption of trans T was stereoselective, (-)-trans T being preferentially absorbed.