Single and multiple dose pharmacokinetics of enteric coated ketoprofen: effect of cimetidine.
The effect of cimetidine on the single and multiple dose pharmacokinetics of enteric coated ketoprofen was studied in 12 healthy volunteers. Each subject completed two 8-day study treatment periods: either ketoprofen alone (100 mg p.o. twice daily), or co-administered with cimetidine (600 mg twice daily). tlag, Cmax, tmax, t1/2, and k for ketoprofen were not significantly different between single and multiple dose administration. AUC of ketoprofen was slightly but significantly larger following multiple (21.2 micrograms.h.ml-1) as compared to single dose administration (19.0 micrograms.h.ml-1). As a result, plasma clearance of ketoprofen was slightly but significantly reduced following multiple dose administration (80.6 ml/min vs 89.3 ml/min). Cimetidine had no effect on the single or multiple dose pharmacokinetics of enteric coated ketoprofen. Total 12-h urinary recovery of ketoprofen (mostly in the form of ketoprofen glucuronide) was 83.5% of the dose following single dose administration and was significantly greater following multiple dose administration (93.1%). Again cimetidine co-administration had no effect on the single and multiple dose urinary recovery. The results of this study show that cimetidine is not affecting the oral pharmacokinetics of enteric coated ketoprofen.
Verbeeck
R K
RK
College of Pharmacy, University of Saskatchewan, Saskatoon, Canada.
Corman
C L
CL
Wallace
S M
SM
Herman
R J
RJ
Ross
S G
SG
Le Morvan
P
P
D000293:Adolescent; D000328:Adult; D002927:Cimetidine / Q000008:administration & dosage*; D004347:Drug Interactions; D006801:Humans; D007660:Ketoprofen / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D008657:Metabolic Clearance Rate / Q000187:drug effects; D010666:Phenylpropionates / Q000493:pharmacokinetics*; D013608:Tablets, Enteric-Coated
D010666:Phenylpropionates; D013608:Tablets, Enteric-Coated; D002927:Cimetidine; D007660:Ketoprofen