Abstract：
:The plasma concentrations and urinary excretions of bisoprolol enantiomers in four Japanese male healthy volunteers after a single oral administration of 20 mg of racemic bisoprolol were evaluated. The AUC(infinity) and elimination half-life of (S)-(-)-bisoprolol were slightly larger than those of (R)-(+)-bisoprolol in all subjects. The metabolic clearance of (R)-(+)-bisoprolol was significantly (P < 0.05) larger than that of (S)-(-)-bisoprolol (S/R ratio: 0.79+/-0.03), although the difference was small. In contrast, no stereoselective in vitro protein binding of bisoprolol in human plasma was found. An in vitro metabolic study using recombinant human cytochrome P450 (CYP) isoforms indicated that oxidation of both bisoprolol enantiomers was catalyzed by the two isoforms, CYP2D6 and CYP3A4. CYP2D6 metabolized bisoprolol stereoselectively (R > S), whereas the metabolism of bisoprolol by CYP3A4 was not stereoselective. The S/R ratio of the mean clearance due to renal tubular secretion was 0.68, indicating a moderate degree of stereoselective renal tubular secretion. These findings taken together suggest that the small differences in the pharmacokinetics between (S)-(-)- and (R)-(+)-bisoprolol are mainly due to the stereoselectivity in the intrinsic metabolic clearance by CYP2D6 and renal tubular secretion.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Horikiri Y,Suzuki T,Mizobe Mdoi
10.1021/js970316dsubject
Has Abstractpub_date
1998-03-01 00:00:00pages
289-94issue
3eissn
0022-3549issn
1520-6017pii
S0022-3549(15)50514-5journal_volume
87pub_type
临床试验,杂志文章abstract：:The conditions of sorption of penicillins and cephalosporins on nonionic macroporous copolymers of styrenedivinylbenzene were evaluated. By increasing the methanol concentration in the eluent, the sorption decreased. Salts exerted little influence on sorption. However, pH exerted a remarkable effect on sorption, and t...
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