Pharmacokinetics in man following oral administration of mexazolam.

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A simple and sensitive method for quantifying 2-chlorophenyl-N-desmethyldiazepam (CND), which is the major metabolite in plasma after administration of mexazolam, has been developed using gasliquid chromatography equipped with electron capture detector (GC-ECD). After extraction with benzene from 2ml of plasma specimens, CND could be quantitated to a lower limit of 0.1 ng/ml. A single oral dose of mexazolam was administrated to ten healthy subjects in order to reveal the pharmacokinetics of mexazolam. The time course of CND in plasma followed the equation of a twocompartment model with an appearance lag time. The mean peak plasma level, 6.80±0.68 ng/ml, was attained at 2.01±0.55 hours after administration of mexazolam, and the apparent elimination half life was 76.4±6.35 hours. The speculated plasma CND profiles reached approximately 90 % of the steady state levels on the 11th day after the initiation of repetitive doses of mexazolam. The calculated average plasma level at steady state, Ca<SUP>ss</SUP><SUB>sv</SUB> following the hypothetical dosage schedule (3 mg of mexazolam administrated per day), was about 65 ng/ml.
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