A. Marzo et al., Pharmacokinetics of diclofenac after oral administration of its potassium salt in sachet and tablet formulations, ARZNEI-FOR, 50(1), 2000, pp. 43-47
This paper reports the results of a pharmacokinetic study involving 24 heal
thy volunteers and designed to characterise the rate and extent of diclofen
ac absorption after the administration of a single dose of diclofenac (CAS
15301-86-5) potassium salt 50 mg in sachet (Voltfast(R)) and tablet (Catafl
am(R)) formulations,
Timed plasma concentrations of diclofenac during a 12-h-period after dosing
were measured by means of HPLC with UV detection at 275 nm and a quantific
ation limit of 10 ng/ml; the method was fully validated for pharmacokinetic
purposes. These plasma concentrations were used to calculate C-max, t(max)
, trapezoidal AUC(0-t) and AUC(0-x) and t(1/2) by means of noncompartmental
analysis C-max and t(max) are the parameters expressing the rate of absorp
tion, wehreas the AUCs reflect the extent of absorption. The rate of absorp
tion with the sachets proved to be very fast, reaching peak values at 10 mi
n in seven subjects and at 15 min in the remaining subjects: mean lime was
13.68 min, with concentrations at 5 min being 38 % of C-max. The average ti
me to peak concentration with the tablets was 53.10 min. The extent of abso
rption of the sachets and tablets was similar with AUC(0-x), values of resp
ectively 1362 and 1214 ng . ml(-1) . h, and a 90 % confidence interval 1.05
-1.20.
The highly soluble potassium salt of diclofenac was rapidly absorbed, espec
ially in its sachet formulation, and thus appears to be an invaluable analg
esic agent that is particularly useful for quick pain relief.