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

2005; Baishideng Publishing Group; Volume: 11; Issue: 12 Linguagem: Inglês

10.3748/wjg.v11.i12.1822

2219-2840

Lianjun Luan,

Systemic Lupus Erythematosus Research

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±0.04h -1 and 0.28±0.06h -1 , of t 1/2 3.56±0.73h and 2.45±0.50h, of T max 2.21±0.45 and 1.75±0.33h, and of Xu 0-24 5.65±0.98 and 2.95±0.62moL 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.