[大鼠肠道中反式曲马多吸收的立体选择性]
[Stereoselectivity in absorption of trans tramadol in rat intestine].
作者信息
Liu Hui-chen, Li Bao-xin, Dun Bin, Wang Yong-li
机构信息
Department of Clinical Pharmacology, Bethune International Peace Hospital, Department of Pharmacology, Hebei Medical University, Shijiazhuang, China.
出版信息
Yao Xue Xue Bao. 2003 Dec;38(12):893-6.
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.
目的
研究反式曲马多（trans T）在大鼠肠道吸收中的立体选择性。
方法
将溶解于 Krebs-Ringer 缓冲液中的 trans T 分别原位灌注大鼠的十二指肠、空肠和回肠。采用高效毛细管电泳（HPCE）法分析灌注液中的 trans T 对映体。
结果
trans T 对映体在大鼠肠道不同节段的吸收分数相似。当 trans T 浓度不高于 40 μmol·L⁻¹ 时，(+)-trans T 的吸收分数低于(-)-trans T。随着 trans T 浓度增加，trans T 对映体的吸收分数降低，且对映体之间吸收分数的差异变得不显著。
结论
trans T 对映体可在大鼠肠道的不同部位被吸收。trans T 的肠道吸收具有立体选择性，(-)-trans T 优先被吸收。
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