Abstract
Felbinac trometamol (trishydroxymethylaminomethane 4-biphenylacetate) is a new water-soluble salt of felbinac currently undergoing clinical evaluation as an intravenous (i.v.) formulation for the treatment of severe post-operative pain. This article reports the pharmacokinetics of felbinac after i.v. administration of felbinac trometamol in Sprague–Dawley rats.
The maximum plasma concentration (C0) and area under the plasma concentration-time curve (AUC) of felbinac administered at doses of 3.36, 8.40 and 21.0 mg/kg felbinac trometamol increased linearly with dose.
Felbinac was highly protein bound (~95%) at plasma concentrations up to 75 μg/ml and extensively metabolized with only small amounts being excreted unchanged in urine (0.318%), feces (0.530%) and bile (0.465%).
4′-Hydroxyfelbinac was the principal metabolite in urine, feces and bile together with felbinac glucuronide, 4′-hydroxyfelbinac glucuronide and sulfate. The majority of the administered dose was excreted in urine (63.6%) mostly as 4′-hydroxyfelbinac. Total drug in urine and feces accounted for about 72% of the dose.
It would appear that felbinac trometamol has the potential to replace lipid-based NSAID formulations and progress to clinical evaluation.
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Acknowledgements
This project was supported by the National Major Special Project for Science and Technology Development of the Ministry of Science and Technology, P.R. China (2009ZX09304-003), the Innovation Fund for Small Technology-based Firms and the Ministry of Science and Technology, P.R. China (08C26214401254).
Declaration of interest
The authors report no declarations of interest.