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口服和静脉注射后大鼠中特他洛尔对映体的药代动力学

Pharmacokinetics of the enantiomers of tertatolol in the rat after oral and intravenous administration.

作者信息

Lave T, Efthymiopoulos C, Van Overloop B, Gairard A, Crambes O, Koffel J C, Jung L

机构信息

Département de Chimie Thérapeutique, Faculté de Pharmacie, Illkirch-Graffenstaden, France.

出版信息

Xenobiotica. 1994 Jun;24(6):561-8. doi: 10.3109/00498259409043259.

DOI:10.3109/00498259409043259
PMID:7975722
Abstract
  1. Plasma concentrations of the two enantiomers of tertatolol were determined by gc/ms. Deuterium labelling of one of the tertatolol enantiomers was used for chiral discrimination. 2. No isotope effects were observed following simultaneous oral administration of tertatolol and [2H9]tertatolol. 3. After intravenous administration of the pseudoracemate or of each enantiomer separately, (+)-tertatolol showed a lower total clearance and volume of distribution, compared to the (-) enantiomer. 4. After oral administration of the pseudoracemate or of each enantiomer separately, no substantial difference in bioavailability were observed between the enantiomers.
摘要
  1. 采用气相色谱/质谱法测定了特他洛尔两种对映体的血浆浓度。其中一种特他洛尔对映体的氘代用于手性鉴别。2. 同时口服特他洛尔和[2H9]特他洛尔后未观察到同位素效应。3. 静脉注射消旋体或各对映体后,与(-)对映体相比,(+)-特他洛尔的总清除率和分布容积较低。4. 口服消旋体或各对映体后,各对映体之间的生物利用度无显著差异。

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