Valle, M. published the artcileAccess of HTB, main metabolite of triflusal, to cerebrospinal fluid in healthy volunteers, Application of 2-Hydroxy-4-(trifluoromethyl)benzoic acid, the publication is European Journal of Clinical Pharmacology (2005), 61(2), 103-111, database is CAplus and MEDLINE.
Triflusal has been shown to exert neuroprotective effects by downregulating mols. considered responsible for the development of Alzheimer’s disease (AD). The aim of this study was to develop a population pharmacokinetic model to characterize plasma and cerebrospinal fluid (CSF) pharmacokinetics of the main active metabolite of triflusal-HTB (2-hydroxy-4-trifluoro-methylbenzoic acid)-in healthy volunteers. Data from two studies were combined. Study A: subjects received single oral doses of triflusal 900 mg. Triflusal and HTB plasma concentrations were extensively measured. Study B: triflusal 600 mg once daily was administered orally for 14 days. HTB plasma and CSF concentrations were determined in healthy volunteers. Population pharmacokinetic modeling was performed using NONMEM. A one-compartmental model with rapid first-order absorption for triflusal and first-order formation of HTB best described plasma concentrations Triflusal elimination rate constant was 50 times faster than that estimated for the metabolite. CSF concentrations of HTB ranged between 0.011 μg/mL and 0.341 μg/mL. A CSF-plasma partition coefficient of 0.002 and a ke0 value of 0.059 h-1 were estimated by means of population modeling. In the present study in healthy volunteers, HTB penetrated into the CSF in a range of concentrations exptl. proven to have protective effects in AD. These concentrations suggest that triflusal could be used in the treatment of central nervous system diseases in doses similar to those used in cardiovascular diseases. Access to the CSF compartment was characterized by a slow equilibrium rate constant and a low CSF-plasma partition coefficient
European Journal of Clinical Pharmacology published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C10H14BNO4S, Application of 2-Hydroxy-4-(trifluoromethyl)benzoic acid.
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