刘会臣, 李保欣, 顿彬, 王永利. 反式曲马朵在大鼠小肠中吸收的立体选择性J. 药学学报, 2003, 38(12): 893-896.
引用本文: 刘会臣, 李保欣, 顿彬, 王永利. 反式曲马朵在大鼠小肠中吸收的立体选择性J. 药学学报, 2003, 38(12): 893-896.
LIU Hui-chen, LI Bao-xin, DUN Bin. Stereoselectivity in absorption of Trans tramadol in rat intestineJ. Acta Pharmaceutica Sinica, 2003, 38(12): 893-896.
Citation: LIU Hui-chen, LI Bao-xin, DUN Bin. Stereoselectivity in absorption of Trans tramadol in rat intestineJ. Acta Pharmaceutica Sinica, 2003, 38(12): 893-896.

反式曲马朵在大鼠小肠中吸收的立体选择性

Stereoselectivity in absorption of Trans tramadol in rat intestine

  • 摘要: 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。

     

    Abstract: AimTo investigate the stereoselectivity in absorption of Trans tramadol (Trans T) in rat intestine. MethodsThe 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. ResultsThe 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 μmol·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. ConclusionTrans 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.

     

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