Effects of microsome enzyme induced by phenobarbarbital on the stereoselectivity of recemic propranolol glucuronidation metabolism / 浙江大学学报·医学版
Journal of Zhejiang University. Medical sciences
;
(6): 7-10, 2004.
Article
in Chinese
| WPRIM
| ID: wpr-341953
ABSTRACT
<p><b>OBJECTIVE</b>To study the stereoselectivity of R-(+) and S-(-)-propranolol glucuronidation and metabolic interaction between R(+)- and S-(-)-propranolol.</p><p><b>METHODS</b>A RP-HPLC analytical method was developed for determination of R-(+)-and S-(-)-propranolol glucuronide (PG) incubated with rat hepatic microsome induced with phenobarbital (PB). The method was applied to investigate the stereoselectivity metabolism of racemic propranolol glucuronidation in vitro.</p><p><b>RESULT</b>In control and PB group, the concentration of R-(+)-PG produced at different substrates was higher than that of S-(-)-PG. Compared with the control, the V(max) and Cl(int) for R(+)-and S-(-)-propranolol increased significantly the K(m) for R(+)-propranolol was elevated, while that for S-(-) propranolol was decreased.</p><p><b>CONCLUSION</b>There is a stereoselectivity in glucuronidation of propranolol in rat hepatic microsome induced with PB and R-(+)-propranolol is preferred. Metabolic interaction between R-(+)-and S-(-)-propranolol exists with a concentration-dependent mode.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Phenobarbital
/
Propranolol
/
Stereoisomerism
/
Microsomes, Liver
/
Enzyme Induction
/
Rats, Sprague-Dawley
/
Metabolism
Limits:
Animals
Language:
Chinese
Journal:
Journal of Zhejiang University. Medical sciences
Year:
2004
Type:
Article
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