Salivary excretion of mexiletine in normal healthy volunteers.
To investigate the kinetics and correlation between serum and saliva levels of mexiletine, serum (total and unbound) and saliva drug concentration-time courses have been analysed in five normal healthy volunteers after administration of a single oral dose (200 mg) of the drug. Mexiletine levels in saliva were always higher than those in serum. The drug concentration-time curve in each sample was analysed according to the non-linear least squares regression program MULTI, for a two-compartment model with first-order absorption. The saliva drug concentration in the post-absorption phase was found to be well correlated with either corresponding serum total or serum unbound drug level in four of the subjects. Although there was a large inter-individual variation in the ratio of saliva to serum drug concentrations as well as in the pharmacokinetic parameters, an almost consistent ratio was obtained in each individual.
Department of Pharmacy, Shimane Medical University Hospital, Izumo, Japan.
Y
Y
Katagiri
S
S
Nagasako
M
M
Hayashibara
K
K
Iwamoto
D000284:Administration, Oral; D000328:Adult; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D008297:Male; D008801:Mexiletine / Q000097:blood / Q000302:isolation & purification / Q000493:pharmacokinetics*; D012463:Saliva / Q000737:chemistry*
D008801:Mexiletine