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PSAPSA
J = P x J = P x !!CCJ : FluxJ : FluxP : Permeability coefficientP : Permeability coefficient!!C : Concentration of drug in donor phaseC : Concentration of drug in donor phase
P = K x D / LP = K x D / LK : Partition coefficientK : Partition coefficientD : Diffusion coefficientD : Diffusion coefficientL : Available path lengthL : Available path length
Slope : J
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P. W. Wertz, et al., J. Invest. Derm., 89, 419-425 (1987).
( )
( )
J = P x J = P x !!CCJ : FluxJ : FluxP : Permeability coefficientP : Permeability coefficient!!C : Concentration of drug in donor solutionC : Concentration of drug in donor solution
P = K x D / LP = K x D / LK : Partition coefficientK : Partition coefficientD : Diffusion coefficientD : Diffusion coefficientL : Available path lengthL : Available path length
4-CH4-CH22 334-CH4-CH22
CHCH 332-CH2-CH22 CHCH 334-CH(CH4-CH(CH 33))225-CH(CH5-CH(CH 33))224-CH(CH4-CH(CH 33))225-CH(CH5-CH(CH 33))22
2929303031313232333334343535
2-CH2-CH33���� CHCH3-CH3-CH33����5-CH5-CH33����2-CH2-CH33����2-CH2-CH33����3-CH3-CH33����3-CH3-CH33����
OthersOthers
OCHOCH 22CHCH 33
OO-Ethylmenthol -Ethylmenthol (1, (1, MET MET ) )
OCHOCH 22CHCH 33 OCHOCH 22CHCH 33
RR
RR
OCHOCH 22 CHCH 33
1166335522
CHCH 33CHCH 22CHCH 33
CHCH 22CHCH 22CHCH 33CH(CHCH(CH 33))22
CHCH 22(CH(CH 22))22CHCH 33CHCH 22(CH(CH 22))33CHCH 33
RR223344556677
44
8899
1010111112121313
CHCH 33CHCH 22CHCH 33
CHCH 22CHCH 22CHCH 33CH(CHCH(CH 33))22
CHCH 22(CH(CH 22))22CHCH 33CHCH 22(CH(CH 22))33CHCH 33
202021212222232324242525262627272828
2,2-di CH 2,2-di CH 333,3-di CH 3,3-di CH 334,4-di CH 4,4-di CH 332,3-di CH 2,3-di CH 332,4-di CH 2,4-di CH 332,5-di CH 2,5-di CH 332,6-di CH 2,6-di CH 333,4-di CH 3,4-di CH 333,5-di CH 3,5-di CH 33
OCHOCH 22CHCH 33
RR141415151616171718181919
di-CHdi-CH 33
RR
CHCH 33CHCH 22CHCH 33
CHCH 22CHCH 22CHCH 33CH(CHCH(CH 33))22
CHCH 22(CH(CH 22))22CHCH 33CHCH 22(CH(CH 22))33CHCH 33
RR
OHOH
ll-Menthol-Menthol
Y.Obata et al., Int.J.Pharm., 198(2000)191-200.
!"#$%#&'()*%+,-+,.,*/.%/$,%),"*%0%1232%&4%56,%7,/,+)8*"9&*.2:!;<2<=>%::!;<2<?2
!
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#!!!
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!$" # % &!
"
#!
'()*+,-+./0102,(+3
'()*+,-+./0102,(+3 45671
45671
%% 689689
:05+;1<+38
:05+;1<+3899
!$" # % &
=+==+=
=+=
=+=
=+=
=+==
=+=
=
>,?./,(>,?./,( @!A+B.80?,(@!A+B.80?,(!$"A+CBD6!$"A+CBD6@!A+B.80?,(@!A+B.80?,(
E)/-07<E)/-07<
F+F+µµµµ11
#%+#%+µµµµ11
GHIGHI
40% Ethanol40% Ethanol0.5% MET/0.5% MET/
40% Ethanol40% EthanolControlControl
-2.5-2.5
0.00.0
2.52.5
(( µµm
)m
)
Administered period (min)Administered period (min)
00 1515
3030 6060
0.5% MET/40%Ethanol0.5% MET/40%Ethanol
@2AB"/"%,/%"'2>%"#$%&'()*2>%%&CD<<EFGHDIJ<<2
DK<<DK=<DH<<DH=<G<<<&!
#%!
L"6,*()B,+%C#)I?F
M,)-,+"/(+,%C
F
NB.&+B"*#,
=O*/,+6"'.
P&Q
R8S$
Symmetric stretchingSymmetric stretchingAsymmetric stretchingAsymmetric stretching
D<1J</0.)/<+3+
9
>,?./,( #A+!KC<?.8,(#%!
#!!
L!
F!
@!
&!!! %M"! %M!! %L"! %L!!
#%!
#!!
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F!
@!
&!!! %M"! %M!! %L"! %L!!
NOP,/O0?7<
:,Q
RH58
@2AB"/"%,/%"'2>%+,-'.'"#$%&'>%8*-+,..2
# % & @"+3?1K#9
I?.<?PH.S+30/O$+)?H.P9
!KC<?.8,(+!$"A
!KC<?.8,(+%A
!
%
@
F
L
>,?./,( ! !$" %# R
6T>,?7<?./0;,?+,-
!K1<?.8,(H?+@!A+<.80?,(
L+8
======
Hexagonal/orthorhombicHexagonal/orthorhombicexisting ratioexisting ratio
RRH/OH/O= = Area of peak at Area of peak at SS=2.4 nm=2.4 nm-1-1
Area of peak at Area of peak at SS=2.7 nm=2.7 nm-1-1
@2AB"/"%,/%"'2>%.'/0,-%'()12>%##"CD<<EFDT=IDTH2
!
%
@
F
L
! !$" @ LNJJ(H70;,?+;1<+389
!KC<?.8,(+%A==
==
=
!
%
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L
! !$" @ L
!KC<?.8,(+!$"A
NJJ(H70;,?+;1<+389
# R6T
@2AB"/"%,/%"'2>%.'/0,-%'()12>%##"CD<<EFDT=IDTH2
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