title: Pharmacokinetic Study of Triflusal in Elderly Subjects After Single and Repeated Oral Administration.
abstract: In this study the single-dose and steady-state pharmacokinetics of unchanged triflusal and its metabolite 2-hydroxy-4-trifluoromethylbenzoic acid (HTB) were studied in 12 elderly subjects treated with a single oral administration of 300 mg triflusal and repeated oral administrations of 300 mg triflusal b.i.d. for 13 days. After a single administration, unchanged triflusal is promptly absorbed (t(max) 0.75 h, C(max) 3.83 &mgr;g/mL) and rapidly depleted from the systemic circulation. Its concentration was measurable only up to 1 to 4 h after administration. The apparent terminal half-life was 0.85 h. HTB proves to be quickly generated from triflusal (t(max) 2.00 h, C(max) 39.88 &mgr;g/mL) and slowly eliminated from the body (t = 54.6 h). With the dose regimen proposed, unchanged triflusal does not accumulate in the body. Conversely, HTB plasma concentration builds up progressively toward steady-state levels of approximately 102 &mgr;g/mL after 4 to 5 d of treatment. No substantial change in peak time, elimination rate constant and half-life evaluated after single-dose treatment was observed on multiple-dose regimen for unchanged triflusal and its metabolite HTB. Therefore, our findings do not indicate a time-dependent pharmacokinetics for triflusal. There were no changes in blood pressure, heart rate or laboratory safety date, i.e., biochemical or hematological profiles.
authors.affiliation: Department of Internal Medicine and Therapeutics, Section of Geriatrics and Gerontology, University of Pavia, Piazza Borromeo, 2, 27100 Pavia, Italy.
authors.forename: E.
authors.initials: E
authors.lastname: Ferrari
authors.forename: G.
authors.initials: G
authors.lastname: Reboldi
authors.forename: P.
authors.initials: P
authors.lastname: Marenco
authors.forename: L.
authors.initials: L
authors.lastname: D'Angelo
authors.forename: F.
authors.initials: F
authors.lastname: Crema
authors.forename: L.
authors.initials: L
authors.lastname: Ambrosoli
authors.forename: A.
authors.initials: A
authors.lastname: Poli
authors.forename: R.
authors.initials: R
authors.lastname: Girardello
authors.forename: D. T.
authors.initials: DT
authors.lastname: Lowenthal