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EC number: 202-509-5
CAS number: 96-48-0
Within the first 2 hours after administration of 4, 40, or 120 mg/kg,
approximately 50% of the administered radiolabel was eliminated as 14CO2.
After 4 hours, approximately 80% of the administered radiolabel had been
eliminated as 14CO2 , and at the end of
the 72-hour recording period a total of 85% to 86% of the administered
dose had been eliminated as 14CO2. 14CO2
accounted for 94% of the radiolabel recovered in excreta. Approximately
4% of the administered radioactivity was excreted in the urine and 0.6%
in the feces over the 72-hour collection period, with the majority of
material excreted within the first 4 hours after administration. At 400
mg/kg, slight saturation of elimination was apparent at the early time
points, as evidenced by somewhat slower formation of 14CO2;
however, at later time points, the total production of 14CO2
was close to that observed at the lower doses.
The distribution of radioactivity was also studied. Seventy-two hours
after administration, a total of 2.28% of the dose remained in the
carcass, with the largest amounts present in liver, muscle, and skin.
The greatest concentration of test article per gram of tissue was in
liver and skin. There was no evidence of bioaccumulation in any tissue.
The results indicate that 1,4-butanediol is rapidly metabolized and
excreted, primarily as CO2, clearly showing that conversion to
gamma-hydroxybutyric acid and succinic acid and processing through the
tricarboxylic acid cycle is the major route of degradation.
According to NTP (NTP, 1996), the current literature documents that both
1,4-butanediol and gamma-butyrolactone are rapidly metabolized to
gamma-hydroxybutyric acid, and the pharmacologic and toxicologic
responses to these chemicals are due to their metabolic conversion to
1,4 -butanediol is rapidly metabolized and excreted as carbon dioxide.
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