A continuous intravenous pyridoxine-infusion (dose = 100 mg PN.HCl; ta
u = 6 h) was given to 10 healthy male volunteers (aged between 23 and
32). Concentration-time curves of B-6-metabolites in urine and blood p
lasma were observed over a period of 240 hours. From these curves biok
inetic parameters were calculated. Renal clearances (ml/min/1.73 m(2))
were 257.5 +/- 92.1 (pyridoxine), 249.8 +/- 48.2 (4-pyridoxic acid),
and 20.1 +/- 6.0 (pyridoxal). Rate constants of elimination (h(-1)) ob
tained by non-linear regression of the excretion curves were 1.231 +/-
0.877 (pyridoxine), 0.314 +/- 0.118 (k(alpha)) and 0.048 +/- 0.070 (k
(beta)) (4-pyridoxic acid), and 0.653 +/- 0.360 (pyridoxal). The main
part of the infused pyridoxine was eliminated in the form of metabolit
es (63.7 +/- 6.4% for 4-pyridoxic acid, 3.3 +/- 0.9% for pyridoxal); o
nly 6.7 +/- 1.8% was excreted unchanged. The proportion of 4-pyridoxic
acid within each miction increased from 53.0 to 100.0%. Our data indi
cate a very effective metabolism of the physiologically inactive pyrid
oxine. An enzyme induction suggested by the increasing proportion of 4
-pyridoxic acid cannot be excluded. Large doses of vitamin B-6 are exc
reted rapidly via the kidney, with the excretion of pyridoxine and 4-p
yridoxic acid being enhanced by tubular secretion.