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Pharmacokinetics of Terazosin Enantiomers in Healthy Chinese Male Subjects

Chirality : the pharmacological, biological, and chemical consequences of molecular asymmetry, v.24 no.12, 2012년, pp.1047 - 1050  

Liu, Man (Department of Clinical Pharmacology, Aerospace Center Hospital, Beijing, People's Republic of China) ,  Zhang, Dan (Department of Clinical Pharmacology, Aerospace Center Hospital, Beijing, People's Republic of China) ,  Yang, Man (Department of Clinical Pharmacology, Aerospace Center Hospital, Beijing, People's Republic of China) ,  Zhao, Ting (Department of Clinical Pharmacology, Aerospace Center Hospital, Beijing, People's Republic of China) ,  Wang, Xiaolin (Department of Clinical Pharmacology, Aerospace Center Hospital, Beijing, People's Republic of China) ,  Zhang, Yanan (Department of Clinical Pharmacology, Aerospace Center Hospital, Beijing, People's Republic of China) ,  Han, Jing (Department of Clinical Pharmacology, Aerospace Center Hospital, Beijing, People's Republic of China) ,  Liu, Huichen (Department of Clinical Pharmacology, Aerospace Center Hospital, Beijing, People's Republic of China)

Abstract

ABSTRACTThe purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of 2‐mg terazosin, the plasma concentrations of terazosin enantiomers were measured over the course of 48 h in 12 healthy subjects. The plasma concentrations of (+)‐(R)‐terazosin at all time points were higher than those of (−)‐(S)‐terazosin. The area under the plasma concentration–time curve (AUC0–∞) and maximum plasma concentration of (+)‐(R)‐terazosin were significantly greater than those of the (−)‐(S)‐terazosin (P < 0.01, respectively). The R/S ratio of AUC0–∞ of terazosin was 1.68. For the first time, it was proven that the pharmacokinetics of terazosin was stereoselective in healthy Chinese male subjects. Chirality 24:1047–1050, 2012. © 2012 Wiley Periodicals, Inc.

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