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P h a r m a c o ıt i n e t ic s t u d ie s
» U n d d in g a n d e m p lo y in g
e rs ta n
p h a rm a c o k in e tic p rin c ip le s c a n
/ in c re a s e th e p ro b a b iı ity o f th e ra p e u tic
/ s u c c e s s a n d re d u c e th e o c c u rr e n c e o f
a d v e rs e d ru g e ffe c ts in th e b o d y .
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Pha rm a c o k in e tic s
» M o le c u ïo r s iz e o n d s fru c tu ro l fe a tu re s,
'
d l lo n iz a tio n
/ » e g e e o
» b in d in g to s e ru m o n d tis s u e p ro te in s
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= M o n y d ru g s a re w e a k a c id s o r b a se s th a i a re p re s e n t
ïn so lu tio n a s b o th th e n o n - lo n iz e d a n d lo n lz e d
s p e e le s .
ı■ Io n lz e d Io w lip id s o lu b ilify ł
e ss b le fo p e n e tra ł
a e ıip id
m e m b ra n e p a ss a ge depe nd o n ı e a k in e s s
o fm e m b ra n e re la te d to m e m b ra n e
'
s
ta n c e
'
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> p H N e g a tiv e lo g a ń fh m o f th e h y d ro g e n io n c o n c e n tra tı
o n
p KQ pH a tw h ic h 5 0 % o f fh e d ru g (w e a k a c id o r b a se
e le c lr o ly fe ) i5 In its io n iz e d (c h a rg e d ) fo rm
= O n ly u n c h a rg e d m o le c u le s o r e lip id s o lu b le
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=
p H N e g a tiv e ïo g a rith m o f th e h yd ro ge n ïo n c o n c e n tra tio n
p H t w h ic h 5 0 % f th e d ru g tw k id b a se
=
p Ko a o e a a c o r
h p H is re o dđ
y c a lc u la te d
a te
Th e ro lio o f n o r Þlo n iz e d to lo n iz e d n ıg
=
d a c
a tio n
k o m th e H e n d e rs o n łosseu»a*Ch e q u
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D R U G A B S O R P T IO N ,
ßï O A V A ï LA B ILIT Y
,
A N D R O U T E S O F A D M IN IS T R A TIO N
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= O N
A B S O R P Tı : m o v e m e n to fa
d ru g fr o m its s ite o f ( ıı治 国 自個 旧
a d m in is tr a tio n in to th e c e n tr a l
c o m p a r tm e n t
= O A V A ILA B IL ITY
Bı fh e fra c tio n a l
.
::, t5 s ite o fa c tio n .
» A d ru g m u s t tr a v e rs e th e
pı
a sm a m e m b ra n e s o f c e lls to
h its s ite o fa c ı
◆
re a c
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M E C H A N IS M S O F D R U G A B S O R P TIO N
)
F A S S IV E T R A N S P O R T
T ıW dSp O RN
/
P ım e « * d w O ıH L p n F a c H H ħd A 0 0
1 Pa
. s s iv e tr a n s p o rt
la .
Po ra c e lï u la r
Tr a n s p o rt
]b D M . u s lo n
ïc .
Fa c ïllta te d d ïfru s Jo n
ıA c tiv e ho n s p o rf
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P a s s iv e tr a n sp o rt A c tiv e tr a n sp o rt
A lo n g c o n c e n tr a tio n a m tio n
g a ln s ıc o n c e n ı
g r a d le n l g ra d ı en l
(l in o m h ig h
ı to ï o w ) (F p o m ı
ow gh)
to h ı
N O 鎖ぽ 姓喾路 N网e! e d s c a r r ie r s
N o ta T l v i e S e¢le c tiv e , s a tu ra bı
e
, r a y ls r e q u tr e d
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S im p le Q ıv e d İ tf u s iç n
W a te r s o u b ı
ı e d r u g (io n iz e d o r a r ) is
po ı re a d ily
a b so r bed v la iıq u e o u s c h a n n e ls o r p o r es In c e ll
m e m b rn n e .
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团团团团■自■■匕
コ自'
サ人
ı
A T P
h O F F
L
區三力
【》 r 니 口
ť .
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D ru ¢\ exı
s ıı
ı tw o fo r m li ı ıı
o ı * r so ı
z ¢d (w a ı ı e &
ıb ı
匡o 豳 ı也 《d fo m s {ııpı d so ıa b 幼 b e q * 出b rı 吲国 .
D 8
n ı ' ı zed +
o ıı ıo * ı
ı o ı
ılim ū
ıO ı
ı b '
lz ¢d ı
a a ılo ıı o r= b a b * o rb a b ı
t
.
ı )io ıi
n u « d /ı z t d fr a c u o
o a ı ıb dt ı a ed
e r ııı
ıa
b3 pı
'
ıd
ı p lia a c c o rd ı
* s ı
o H ıd e n o ı
eı -
U b i«
a \\e ı h
l= ı «d / lo m cd
ı
pK r pı o g pro ı n ı
o ı ıp m
ıo ı
ı -
-
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T h e io n iz a t io n o fa w e a k a c id H A is g iv e n
◆ th e e q a ti
lo n
P村 コ
p K a + lo g
iĤ 西丁
c ia t io n c c m s ta n t o f th e w e a k le c t r o ly t e
e If t h e
c o n c e n tr a t io n o f io n iz e d d m g [ A ] s e q u a l to
l
n tr a tio n d r u g [IM
c e o J
Ł = łn ı- - n Fh n p
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A c tiv e tn ın s p o rl C a r r ie m e d la t e d
fa c llM a t e d d lf 【
u s lo n
A g a in s t c o n c e n tr a tio n a lo n g c o n c e n tr a tio n
gra dı en t g r a d ie n t
(F r o n ıı
ow to M g h ) (F r o m h ı
gh to ı
ow )
N e e d s c a r r ie r s N e e d s c a r r ie r s
S e le c tiv e , s a tm a b le S e le c tlv e9 sa ïu ra b le
r e q u ir e d
E n e iw ls re q a ir e d N n erw ls
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寧 島鹼 阁 国道 唧 塒 印壮卿卅 刨餬 M 姻
切笋紐帥 囀 P 1 目 回国团团团国
。
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ßS O R P T IO N
= th e ra te cm d
e ffrc le n c y o f
c rb s o rp fio n dep e n d o n
lĄh e
,
ro u fe o f
d m in is trc ttio n
k
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= M o s t d ru g s a b d fr o m th e
s o rb e
G l tr a c t e n te r th e p o r ta l
ć jr c u la tio n a n d e n c o u n te r th e
Ilv e r b e fo re th e y a r e d is lń b u te d
in fo th e g e n e r a l c ire u la tio n .
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= M o s t d ru g s a b s o r b e d fr o m th e
G I tr a c t e n fe r th e p o r ta l
c ir c u la tio n a n d e n c o u n te r th e
liv e r b e fo
fh e y a r e d is tń b u te d
re
in to th e g e n e r a l c irc u la tio n .
th e s y s te m ic c kc u la tio n .
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O R A L A D M IN S T R A T IO N
し 스出
ー
ー
く 照
= s d u lio n s u s p e n s io n o r s o lid d o s a g e
.
(ta b .
c a p )
= m o stc o m m o n m e th o d sa le 5 t m o s t c o n v e n ie n t m o sr
e c o n o m ic a l
d e s tr o y e d b y g a s tr ic s e c re fio n s I
s
o w p h a n d th a t.
c o a tin g p ï e v e n ïs d is s o lu fio n m th e o c id lc
-
g a s tr ic
c o n fe n fs .
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P TR A N S D E R M A L A B S O R F
hy
d r ol ed sk in mo r e pe r me o b ï e t ho n dr y sk i n
i tin e (fo b a c c o sm o k in ç
: fe n t o n y l p a tc h n c o -
» e g
fo ris
. .
, Ļ v i th d ra w al) N itro g ïy c e ń n e fo
,
r a n g in a p e c ,
e n ï th e ra py
e s fï o g e n & te s to s te r o n e r e p ïo c e m ・
십 自 ん园 区きら ー ― ―
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P A R E M E R A L A D M JN IS TR A TIO N
=
S u b c u t a IM O P » i o R S i m p l e ąg /(
d f f a lo n g th e g p o đ e r ıī lr «m d m g
« le p o ī Io p ł
o sm o
-
ıı
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M t» e p r o le m d
e o w w o u n o
:I Y P O t A しê U r 】a j 4
1
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Ļ C N S & C E R E B R 0 5 ĦN A L F L D
H H -t
°
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C N S & C E R E B R O S P IN A L F L U ID {C SF)
7
= D ru g p e n e h a tio n d e p e n ds o n
tr o n s c e lł
u la r ra th e r th a n p a ra c e llu la r
o p h ilic a d ru g th e m , o re
:ro s s łh e b lo o d b ra in -
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