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EC number: 609-066-0
CAS number: 35123-06-9
In the rat skin model,
the highest penetration potential was measured for
N,N-dimethyldecanamide (Kp = 9.26 and 10.05 x 10³ cm/h). Smaller
as well as bigger molecules had a lower penetration rate (e.g.
N,N-dimethylhexanamide: Kp = 1.63 x 103cm h-1);
= 3.01 x 103cm h-1).
The article leads to
the following results for ibuprofen (IBU):
The flux of ibuprofen
(IBU) is the highest if C8- (136µmol/(cm2h))or
C10-dimethylamides (159µmol/(cm2h)) are added. Only the
(NMPo) lead to a higher flux (203µmol/(cm2h)).
The lag time for
IBU is not affected by C8 (3.4h) or C10 -dimethylamides
(3.3h) but also
not by the reference NMPo (3.4h) [ to compare 50% PG (3.1h) and buffer
Flux ratio was
increase to 2.3 and 1.9 fold for C8 and C10 FADMA respectively
(calculated against 50% PG).
Solubility of IBU was
only increased 9 or 15% by C10 and C8 FADMA, respectively, while the
solubility is increased 280% by NMPo.
And to the following
for naproxen (NAP):
The flux of NAP is ten
times higher if 1% C10 FADMA is added and seven times higher if C8 FADMA
is added. For NMPo (10%) only a 2 fold increase could be observed.
The lag time for NAP
is not affected by C8 (2.9h) or C10 (3.3h) whereas NMPo decreases the
lag time to 4.9h [to compare 50% PG (2.9h) and buffer (3.6h)].
Flux ratio was
determined for C8- and C10 -dimethylamide as 7 and 10 fold,
Solubility of NAP is
increased 57% and 30% if C8- or C10 -dimethylamide is added, but NMPo
increases the solubility by 324 %.
Determination of the
partition coefficients shows an 3.7 fold (dry) and 5.5 fold (dry)
increase compared to 50% PG (propylen glycol).
"n-Alkanoic N,N-dimethylamides were found to act as penetration
enhancers for the transport of ibuprofen and naproxen from
suspensions in 50% aqueous propylene glycol vehicles across rat
skin. Stripped skin and separated dermis were used to establish
the maximum potential for enhancement and comparisons with
established enhancers such as azone and N-methylpyrollidone were
undertaken. Greatest enhancement was observed with naproxen but
both drugs demonstrated a bell-shaped dependence on the alkyl
chain length of the enhancer. Maximum effect was observed with
N,N-dimethyloctanamide and N,N-dimethyldecanamide. Measurement of the
skin-vehicle partition coefficients indicated that the partition of the
drug into the skin was also maximal when these enhancers were
incorporated into the vehicle. Permeation studies monitoring the flux of
enhancer indicated that these compounds also penetrated the skin most
effectively. In contrast, the enhancers had little effect on delivery
from liquid paraffin vehicles."Irwin, W. J.; Sanderson, F.
D.; Po, A. Li Wan
Percutaneous absorption of ibuprofen and naproxen: effect of amide
enhancers on transport through rat skin International Journal of
Pharmaceutics (1990), 66(1-3), 243-52
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