Dose Proportionality of Bisoprolol Enantiomers in Humans After Oral Administration of the Racemate

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Abstract
Dose proportionality of racemic bisoprolol and the stereoselectivity of its enantiomers were studied after single oral dosing of 5 to 40 mg of bisoprolol hemifumarate in eight healthy male volunteers in an open‐label, randomized, four‐way cross‐over trial. There were dose‐proportional increases in mean peak plasma concentration (Cmax) and area under the plasma concentration versus time curve (AUC) values for the racemate and the individual enantiomers. No statistically significant differences were detected between the mean half life (t1/2), Cmax, and time to reach Cmax (tmax) of the R‐ and S‐isomers at each of the four dose levels studied. These findings support dose proportionality and absence of stereoselective pharmacokinetics for bisoprolol in the dose range studied.