Stereoselective Pharmacokinetics of Bisoprolol After Intravenous and Oral Administration in Beagle Dogs

摘要: The stereoselective pharmacokinetics of bisoprolol, a highly β1-selective adrenoceptor blocking agent, was studied in dogs. After intravenous and oral administration the racemate, there difference plasma concentration between S(−)- R(+)-bisoprolol. area under curve (AUC) versus time S(−)-bisoprolol ∼1.5 times higher than that R(+)-bisoprolol, elimination half–life ∼1.4 longer However, no differences were observed volume distribution, absolute bioavailability, renal clearance two enantiomers. protein binding also same as R(−)-isomer. No chiral inversion or enantiomer–enantiomer interaction observed, when enantiomers solely administered via route. comparison oxidative metabolic rate using dog liver microsomes demonstrated metabolite more slowly formed from Consequently, we concluded R(+)-bisoprolol caused disposition bisoprolol