Baicalin, baicalein, wogonoside and wogonin are flavone constituents of Scutellariae Radix with various beneficial biological activities. The purpose of this study was to investigate the urinary pharmacokinetics of these flavones after oral administration of Scutellariae Radix commercial powder. Ten healthy male volunteers received a dose of 5.2 g commercial powder (comparable to 9 g crude drug), respectively. The concentrations of baicalin, baicalein and wogonin in the commercial powder as well as their metabolites in urine were assayed by HPLC method. The glucuronides and sulfates of baicalein and wogonin in urine were hydrolyzed with b b-glucuronidase and sulfatase, respectively. Our results showed that the mean cumulated renal excretion of baicalein glucuronides and sulfates were 43.1؎4.5 m mmol (2.9% of dose) and 64.8؎6.3 m mmol (4.3% of dose), respectively, whereas wogonin glucuronides and sulfates were 21.6؎2.0 m mmol (5.9% of dose) and 20.7؎1.7 m mmol (5.7% of dose), respectively. The result indicated that the renal excretion of conjugated metabolites of wogonin (11.6% of dose) were higher than that of baicalein (7.2% of dose). The baicalein sulfates was predominant than the corresponding glucuronides, whereas wogonin sulfates was comparable to the corresponding glucuronides.

To measure naringin/naringenin absorption of a decoction prepared from the pericarps of Citrus grandis and to investigate the effect of honey on naringin/naringenin absorption, six healthy males received 200 mL decoctions of untreated and honey-treated Pericarpium Citri Grandis in a randomized crossover design. The absorption was measured by renal recovery of naringenin glucuronides/sulfates over 48 hours. The contents of naringin/naringenin in 200 mL decoctions of untreated and honey-treated Pericarpium Citri Grandis were determined to be 261.5/23.8 mumol and 303.3/11.6 mumol, respectively. The mean cumulated renal excretion of naringenin glucuronides/sulfates after intake of these two decoctions were 74.8 mumol (26.2% of dose) and 49.8 mumol (15.8% of dose), respectively. Paired Student's t-test showed that the difference of the total renal recovery of naringin/naringenin between the two decoctions was significant. The results indicated that honey significantly reduced naringin/naringenin absorption by 33.4% in humans and suggested that honey treatment might alter the efficacy of Pericarpium Citri Grandis.