The excretion of hydroxyamylobarbitone in man after oral administration of amylobarbitone and hydroxyamylobarbitone

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Abstract
The excretion of hydroxyamylobarbitone in man has been measured over six days after an oral dose of 200 mg of sodium amylobarbitone. The biological half-life of hydroxyamylobarbitone determined from “Sigma-minus” plots ranged between 16·8 and 22 h in seven subjects, in another subject the half-life was 34·4 h. The effects of increasing urine flow on the amount of hydroxyamylobarbitone excreted after ingestion of 200 mg of sodium amylobarbitone were assessed. A subject normally excreting 34% of the dose as hydroxyamylobarbitone excreted 45% of the dose as metabolite while taking chlorothiazide as a diuretic. With the same subject taking increased fluids to produce a greater urine flow 41% of the dose was excreted as hydroxyamylobarbitone. Hydroxyamylobarbitone is not bound to plasma proteins and when an aqueous solution of 50 mg of hydroxyamylobarbitone was taken by mouth, 57% of the dose was eliminated in the first 8 h and 91% in the first 24 h. The half-life for ingested hydroxyamylobarbitone was 5·7 h, showing that the rate of elimination of this metabolite is faster than its rate of formation when amylobarbitone is ingested.

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