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

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 enantiomar separately, no substantial difference in bioavailability were observed between the enantiomers.