Key result
Increasing single doses of diflunisal from 100 mg to 750 mg significantly decreased total plasma clearance from 14.4 to 8.7 ml/min due to saturation of acyl glucuronide formation.
Why the study?
Does the dose of diflunisal affect its glucuronidation and sulphation kinetics in healthy volunteers?
Population
6 healthy volunteers
Comparison
Diflunisal single doses vs Comparison across different dose levels
Design
Other
Authors
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Suggests caution with higher diflunisal doses due to reduced clearance; leaves open effects on efficacy and safety in patients.
Does the dose of diflunisal affect its glucuronidation and sulphation kinetics in healthy volunteers?
Diflunisal exhibits dose-dependent plasma clearance primarily due to the saturation of acyl glucuronide formation.
Loewen et al. (1988) studied Healthy volunteers (n=6). Diflunisal was evaluated on Glucuronidation and sulphation kinetics (urinary recovery and plasma clearance). Increasing single doses of diflunisal from 100 mg to 750 mg significantly decreased total plasma clearance from 14.4 to 8.7 ml/min due to saturation of acyl glucuronide formation.
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