Sc. Chi et al., EFFECT OF PENETRATION ENHANCERS ON FLURBIPROFEN PERMEATION THROUGH RAT SKIN, International journal of pharmaceutics, 126(1-2), 1995, pp. 267-274
To increase the skin permeation rate of flurbiprofen, fatty acids and
urea were added in propylene glycol vehicle containing 1% flurbiprofen
. The enhancing effects of these compounds on the skin permeation of f
lurbiprofen were evaluated using Keshary-Chien diffusion cells fitted
with excised rat skins. Unsaturated fatty acids increased the skin per
meation rate of flurbiprofen 6.5-17.5 fold compared to the control veh
icle without enhancer, while saturated fatty acids did not show any si
gnificant increase. Although the addition of urea in the vehicle decre
ased the skin permeation rate of flurbiprofen, the mixture of oleic ac
id and urea showed a significantly higher permeation rate than oleic a
cid alone. It was coincident with the results obtained with the plasma
concentrations of flurbiprofen determined after the transdermal appli
cation of propylene glycol vehicle containing them. AUC and C-max of t
he vehicle containing the mixture were increased 2.3 and 2.5 fold, res
pectively, whereas each parameter of the vehicle containing oleic acid
only was increased 1.7 fold compared to those of the control vehicle.