Izquierdo, Inaki published the artcileComparative bioavailability study of triflusal oral solution vs. triflusal capsules in healthy subjects: a single, randomized, two-way cross-over, open-label phase I study, Formula: C8H5F3O3, the publication is Arzneimittel Forschung (2010), 60(1), 36-41, database is CAplus and MEDLINE.
Triflusal (CAS 322-79-2) is an antiplatelet agent that irreversibly acetylates cyclooxygenase isoform 1 (COX-1) and therefore inhibits thromboxane biosynthesis. The main metabolite of triflusal, 2-hydroxy-4-trifluoromethyl benzoic acid (HTB), possesses also antiaggregant activity. Recently a new oral 600 mg (10 mL) solution form of triflusal has been developed. The purpose of this clin. trial was to study the relative bioavailability of the new oral solution of triflusal vs. the capsules formulation, both administered as a single dose. This was a randomized, two-way, cross-over, open-label, single-site phase I clin. trial, in 24 healthy volunteers who received triflusal as 600 mg oral solution and as two 300 mg capsules in a single administration separated by a washout period of at least 17 days. Blood samples were collected and plasma concentrations of HTB were measured. Pharmacokinetic parameters used for bioequivalence assessment included AUC0-t, AUC0-inf and Cmax. The formulations were considered bioequivalent if the geometric mean ratios of AUC0-t, AUC0-inf and Cmax were within the predetermined equivalence range (80% to 125%). Tolerability was based on the recording of adverse events (AEs), phys. examination, ECG and laboratory tests. The parameters for bioequivalence, mean [SD] values were as follows: AUC0-t (μg/h/mL): 3574.08 [628.17] for triflusal oral solution and 3901.78 [698.43] for triflusal capsules; AUC0-â?/sub> (μg/h/mL): 4089.21 [842.54] for triflusal oral solution and 4471.33 [905.93] for triflusal capsules; Cmax (μg/mL): 91.24 [12.88] for triflusal oral solution and 88.61 [13.46] for triflusal capsules; Cmax/AUC0-â?/sub> (h-1): 0.03 (0.00) for triflusal oral solution and 0.02 (0.00) for triflusal capsules. The 90% confidence intervals for the ratio exptl./control by anal. of variance after log transformed AUC0-â?/sub>, AUC0-t, and Cmax were within 80% to 125%. Similar results were found for the data without log transformation. All adverse events were of mild or moderate intensity and all subjects recovered. Nine and 12 subjects reported at least one adverse event during treatment with triflusal oral solution and with triflusal capsules, resp. The most frequently reported adverse events were headache and dizziness. It was concluded that the 600-mg solution of triflusal appeared to be bioequivalent to the reference formulation capsules. Both formulations were well tolerated.
Arzneimittel Forschung 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 C8H5F3O3, Formula: C8H5F3O3.
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