PHARMACOKINETICS OF PEMOLINE IN PLASMA, SALIVA AND URINE FOLLOWING ORAL-ADMINISTRATION

1 Pemoline concentrations were measured in plasma and saliva following a single oral dose (37.5 or 50.0 mg) to healthy volunteers. In addition urinary excretion rates and cumulative urinary excretion of the parent compound and its oxazolidinedione metabolite were determined. 2 The plasma curves exhibited a mean elimination half‐live of 11.0 +/‐ 1.2 h (n=4). Peak levels were reached at 2.7 +/‐ 0.6 h (n=4). The saliva concentrations were about 50% lower than the corresponding plasma concentrations during the elimination phase. During the absorption phase irregularities in the saliva to plasma concentration ratios were observed. 3 In urine 47.0 +/‐ 8.4% of the dose (n=6) administered was excreted as unchanged drug and only 3.7 +/‐ 0.8% (n=3) as the oxazolidinedione metabolite. Urinary half‐lives were slightly shorter than the corresponding plasma half‐lives. 1979 The British Pharmacological Society