Stereoselective urinary excretion of S-(-)- and R-(+)-propranolol glucuronide following oral administration of RS-propranolol in Chinese Han subjects

doi:10.3748/wjg.v11.i12.1822

Advanced Search

BPG is committed to discovery and dissemination of knowledge

Home / Archive / Volume 11, Issue 12

This Article

Citation of this article

Corresponding Author of This Article

Article-Type of This Article

Open-Access Policy of This Article

Times Cited Counts in Google of This Article

Number of Hits and Downloads for This Article

Total Article Views (2555)

All Articles published online

The chart showing PDF series, HTML series, Figures (1-2) series, Tables (1-2) series.

Item

Count

PDF

260

HTML

1944

Figures (1-2)

187

Tables (1-2)

164

Sum=2555

Mar 28, 2005 (publication date) through Nov 27, 2024

Times Cited of This Article

Times Cited (10)

Journal Information of This Article

Publication Name

World Journal of Gastroenterology

ISSN

1007-9327

Publisher of This Article

Baishideng Publishing Group Inc, 7041 Koll Center Parkway, Suite 160, Pleasanton, CA 94566, USA

Brief Reports

World J Gastroenterol. Mar 28, 2005; 11(12): 1822-1824
Published online Mar 28, 2005. doi: 10.3748/wjg.v11.i12.1822

Stereoselective urinary excretion of S-(-)- and R-(+)-propranolol glucuronide following oral administration of RS-propranolol in Chinese Han subjects

Lian-Jun Luan, Qing Shao, Jian-Yin Ma, Su Zeng

Qing Shao, Su Zeng, Lain-Jun Luan, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310031, Zhejiang Province, China

Jian-Yin Ma, College, Zhejiang Ocean University, Zhousan 316000, Zhejiang Province, China

Author contributions: All authors contributed equally to the work.

Correspondence to: Professor Su Zeng, Department of Pharmaceutical Analysis and Drug Metabolism, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310031, Zhejiang Province, China. zengsu@zju.edu.cn

Telephone: +86-571-87217203 Fax: +86-571-87217086

Received: May 25, 2004
Revised: May 27, 2004
Accepted: June 17, 2004
Published online: March 28, 2005

Abstract

AIM: To study the stereoselectivity of phase II glucuronidation metabolism of side-chain propranolol in Chinese Han population.

METHODS: Sixteen adult Chinese Han volunteers with an average age of 20 years were given a single oral dose of 20 mg racemic propranolol. Human urine at indicated time after administration was collected and S-(-)-propranolol glucuronide and R-(+)-propranolol glucuronide were determined simultaneously by using RP-HPLC.

RESULTS: The mean values of k were 0.19±0.04 h^-1 and 0.28±0.06 h^-1, of t_1/2 3.56±0.73 h and 2.45±0.50 h, of T_max 2.21±0.45 and 1.75±0.33 h, and of Xu^0-24 5.65±0.98 and 2.95±0.62 μmoL for S-(-)- and R-(+)-propranolol glucuronide, respectively. The cumulative excretion percentages in urine of doses were 14.7±2.46% and 7.68±1.60% for S-(-)- and R-(+)-propranolol glucuronide, respectively. The results showed the elimination rate constant k of S-(-)-propranolol glucuronide was less than that of R-(+)-propranolol glucuronide; and the elimination half-life (t_1/2), T_max and the cumulative excretion amount(Xu^0-24) of R-(+)-propranolol glucuronide were significantly less than that of S-(-)-propranolol glucuronide.

CONCLUSION: The propranolol glucuronidation of the side-chain undergoes stereoselective excretion in Chinese Han population after an oral administration of racemic propranolol.

Keywords: Stereoselectivity; Excretion; Propranolol enantiomer; Glucuronidation