1. ȯڿ .
1) Ǵ п
ι( ) ִ ȯ
2) ⸳ ȯ( ȭ ִ.)
3) ȯ( ִ.)
4) Ӻ Ǵ ӽϰ ɼ
ִ
2. ȯڿ
1) ȯ( ִ.)
2) (ڿ )
3) PDE5(phosphodiesterase-5) ȯ(ȣۿ )
4) CYP3A4 ȯ(ȣۿ )
5) а ȯ(ȣۿ
6) 1- ȯڴ ʴ Ģ ϳ, Ư
ʿ 쿡 Ͽ Ѵ.(⸳ Ͼ ִ.)
7) 财ǽ ִ ȯڴ
ʴ Ģ ϳ, Ư ʿ 쿡 Ͽ Ѵ.
3. ̻
1) Žνſ꿰
缺 ȯ 482 12ְ
ӻ迡 Ǿ.
0.4mg 155 ϰ ̻ κ谨(1.94%),
(1.94%), (1.94%), (1.29%), ȭҷ(1.29%), (1.29%), (1.29%), (1.29%) ̾. ΰ踦 ̻
2, 2, 1, ȱ 1,
谨 1,
1, 1, 1, 1, 1̸, ȱ(ߵ)
̻ Ÿ.
ǥ ӻ迡 ΰ ü 482 ( 162, Žνſ꿰 0.2mg 165, Žνſ꿰 0.4mg 155)
̻ 1% ̻ ǰ ̻
̴.
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Žνſ꿰 (N=320)
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ü
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0.4mg
(N=155)
N(%)
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0.2mg
(N=165)
N(%)
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(N=162)
N(%)
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(N=482)
N(%)
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ȭ
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3 (1.94%)
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0 (0%)
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1 (0.62%)
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4 (0.83%)
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3 (1.94%)
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1 (0.61%)
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0 (0%)
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4 (0.83%)
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2 (1.29%)
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0 (0%)
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0 (0%)
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2 (0.41%)
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ȭҷ
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2 (1.29%)
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0 (0%)
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2 (1.23%)
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4 (0.83%)
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|
|
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2 (1.29%)
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0 (0%)
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0 (0%)
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2 (0.41%)
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Ű
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3 (1.94%)
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1 (0.61%)
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1 (0.62%)
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5 (1.04%)
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2 (1.29%)
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0 (0%)
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0 (0%)
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2 (0.41%)
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ı
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1 (0.65%)
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2 (1.21%)
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0 (0%)
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3 (0.62%)
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2 (1.29%)
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0 (0%)
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0 (0%)
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2 (0.41%)
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Ǻ
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0 (0%)
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2 (1.21%)
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0 (0%)
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2 (0.41%)
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2) Ʒ õ Žνſ꿰 0.2mg ӻ 迡
ٰŷ ̴.
(1) ǽ, ǽĻ( Ҹ) : Ͽ
ϴ ϰ ǽĻ Ÿ Ƿ ϰ, ̻ Ÿ 쿡
ϰ óġ Ѵ.
(2) ŽŰ : , ̻,
⸳ , , , Ű, Ҹ, , (Ҹ), (Ҹ) Ÿ ִ.
(3) ȯ : , , ⸳
, ɰ, Ÿ ִ.
(4) ι : , , ε巯
Ÿ Ƿ ̷ Ÿ 쿡 ؾ Ѵ.
(5) ȭ : , , κ谨, ߰, , Ŀ, , , , ġ, ְ Ÿ ִ.
(6) , Ȳ( Ҹ) : AST , ALT , Ȳ Ÿ 찡 Ƿ, ϰ ̻ Ÿ 쿡 ϴ óġ Ѵ.
(7) Ÿ : εκ ۿ, ű°, ڸ, , , DZ, ̰̻, , ӹ߱, , , , , , εο, ħ , κ, , ,
ȫäı(Intraoperative Floppy Iris Syndrome), þ帲, ð, ȫ, ŻǺο
Ÿ ִ.
(8) (ʼ : 3,720) Ÿ
̻ , δ Ȯ ʴ. :
ȣ, , , ̸(ĸ .).
(9) ܱ(̱) Ÿ ̻ , ̴ ڹ ŷڼ ִ ΰ Ǵ ̷ ƴϴ. ̱ 1) ̻ ߴ뼺
2) Ƚ 3) ΰ ٰŷ Ͽ ̻
ǻ Ͽ., Լ Ǻȯ, , ˷ ε巯, ɰ, , Ǻιڸ, , , 幰
ӹ߱ Ǿ. 1- ϰ ְų
ߴ Ϻ ȯڿ 鳻 Ǵ 쳻 ϴ ȫäı(IFIS)
˷ ִ ı Ǿ.
3) Žνſ꿰 0.4mg
ɻ縦 Ͽ 6 682
ǽ , ̻ ΰ 10.26%(70/682,
77) Ǿ. ΰ
ߴ ̻ʴ Ʒ ǥ Ͽ, ΰ踦 ߴ ̻
ʾҴ.
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ΰ ߴ ̻
0.73%(5/682, 6)
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ʰ(0.11%̸)
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㵵 ȯ
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-ݰ
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ȸı
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ı
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ı ()
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Ż
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忰
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ȯ
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ϰ
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, ΰ ̻ʿ ΰ踦
̻ ǥ Ͽ.
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ΰ
̻
4.69%(32/682, 37)
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ΰ踦 ̻
0.73%(5/682, 5)
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ʰ(0.11%̸)
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ȯ
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ŰἮ, , 财, , Űμ汤, ΰἮ
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财
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, 忰, , Խǿ,
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Խǿ, â*
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ı ()
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߱, ߱, Ż,
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߱
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ȯ
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, , ż
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ż, ̹*, *
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ʽŰ
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, ô, Ų
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-ݰ
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, ȸı
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-
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㵵 ȯ
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-
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Ÿ
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ڿߵ
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-
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к ȯ
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-
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ȯ
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-
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ı
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-
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Ż
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-
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ɱ, ɳ, ɸ, Ǹ
ȯ
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-
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Ϲ ȯ
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-
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ȯ
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ȯ
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-
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ȯ
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ϰ
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-
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ȣ ȯ
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ħ
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-
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* Žνſ꿰 0.4mg 漺ʸ, ,
漺ĸ
4. Ϲ
1)
ϰ ǹǷ ؾ Ѵ.
2) ⸳() Ƿ üȯ кȭ Ѵ.
3) ġ ο
ƴ϶ ӿ Ͽ Ǵ ȿ ϴ 쿡 ٸ óġ ؾ Ѵ.
4) Ÿ Ƿ
۾̳ ڵ ۾ ϴ 쿡 Ǹ ȯѾ Ѵ.
5) 迡 ܹ
Ÿ Ǿ.
6) ϰ ߱ϴ
ϰ, ȯ ϹǷ ִ Ͽ Ѵ.
7) 輺 ٸ - .
8) 幰 ٸ 1- ӹ߱ õȴ. ӹ߱ ´
óġ ߱Ҵ ߱ Ƿ ǻ ̷ ɰ ȯڿ ˷ Ѵ.
9) 1- ϰ ְų ߴ Ϻ ȯڿ 鳻 Ǵ 쳻 ϴ ȫäı(IFIS) Ǿ. ȰǴ ȫä (irish hook), ȫäȮ(irish dilator ring) Ǵ
ź(viscoelastic substance) ַ ϴ ־
ȭ غؾ Ѵ.
10) Ƹ̵ ˷
ȯ( ˷ ʰ Ǿ.
ȯڰ ſ ˷⸦ ٸ, ǰ ʿϴ.)
5. ȣۿ
1) а ȯڴ ⸳
ɷ ϵǴ 찡 , а ⸳ Ÿ Ƿ ϴ
Ѵ.
2) ۿ PDE5 (ǵʽƮ꿰,
ٵʿ꿰 ) PDE5
̿ϼ аۿ ִ. PDE5
ɼ ִ.
3) ٸ - ȣۿ , ȣۿ Ǹ, аۿ ̷ ִ.
4) øƼ ȣۿ뿡
û(25 % ) AUC(44 % ) ߿ ȭ ŸǷ øƼ
Ѵ(Ư 0.4 mg ̻ 뷮 ).
5) ĸ ȣۿ
ѵ in vitro, in vivo 迡 п ̸ Ƿ Ѵ.
6) ǰ ൿ 迡
CYP3A4 Ǵ CYP2D6
Ǿ. ڳ(CYP3A4
) Žνſ꿰 0.4 mg
Žν Cmax AUC 2.2, 2.8 Ͽ.
CYP2D6 籺(poor
metabolizer) CYP3A4 Žνſ꿰 Žν
ɼ ִ. CYP2D6 (polymorphism)
Ϲ ˷ ʱ Žνſ꿰 CYP3A4 (ڳ, Ʈڳ, ڳ, ŬƮθ̽, ε, dz, 䳪, )
Բ ؼ ȵȴ. ߵ CYP3A4 (Ʈθ̽, ÷ڳ, Ƽ, Ĺ) Žνſ꿰 Ѵ. ķϼƾ(CYP2D6 )
Žνſ꿰 0.4 mg Žν Cmax AUC 1.3, 1.6
Ͽ.
6. Ӻ ο
ʴ´. ȿ Ȯ
ʾҴ.
7. Ҿƿ
ҾƸ ʴ´. 18 Ҿƿ ȿ
Ȯ ʾҴ.
8. ڿ
ߵ ȯڿ 뷮 ʿ ʴ.
ȯ (Creatinine Clearance 30mL/min ̸) ȿ ʾҴ.
9.
1) PTP PTP κ Ѵ. PTP ϰ , ܴ κ ĵ
õ ݵ(̰) պ
Ѵٴ ִ.
2) ̹Ƿ þ
ʵ ȯڿ ǽŲ( ).
10. ǻ
1) ʴ
Ѵ.
2) ٸ ٲپ ִ
ǰų ǰ 鿡 ٶ Ƿ ̸ Ѵ.
11. Ǿǰ 1
. Žü0.4и(Žνſ꿰)[()ٻ] ѹŽĸ0.4и(Žνſ꿰)[ѹ̾ǰ()] 22 1 Ǵ 1 ĸ ǰ ο ȸ 汸 Ͽ 29() 29() Žν , ġ(AUCt, Cmax) αȯϿ óϿ
, ġ 90%ŷڱ log0.8 log1.25̳μ Ͽ.
<>
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AUC0-36hr
(nghr/mL)
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Cmax
(ng/mL)
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Tmax
(hr)
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t1/2
(hr)
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ѹŽĸ0.4и
(Žνſ꿰)
[ѹ̾ǰ()]
|
151.148.4
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12.163.06
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5.00(2.006.00)
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9.182.13
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Žü0.4и
(Žνſ꿰)
[()ٻ]
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160.859.6
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12.984.19
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5.00(3.006.02)
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8.941.73
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90% ŷڱ*
( : log0.8 ~ log1.25)
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log0.9786~
log1.1188
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log0.9836~
log1.1199
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-
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-
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AUCt,Cmax,t1/2:հǥ, Tmax :
߾Ӱ(), n=29
AUClast :
ð ߳
ð ߳-ðϸ
Cmax :
ְ߳
Tmax :
ְ߳ ð
t1/2 :
ҽ ݰ
* ġ αȯ ġ 90% ŷڱ
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<>
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AUC0-36hr
(nghr/mL)
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Cmax
(ng/mL)
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Tmax
(hr)
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t1/2
(hr)
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ѹŽĸ0.4и
(Žνſ꿰)
[ѹ̾ǰ()]
|
129.251.1
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9.2183.162
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5.00(4.0012.00)
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9.761.99
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Žü0.4и
(Žνſ꿰)
[()ٻ]
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130.353.0
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9.7682.969
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5.00(2.007.02)
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10.623.86
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90% ŷڱ*
( : log0.8 ~ log1.25)
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log0.9666~
log1.0539
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log0.9972~
log1.1533
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-
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-
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AUCt,Cmax,t1/2:հǥ, Tmax :
߾Ӱ(), n=29
AUClast :
ð ߳
ð ߳-ðϸ
Cmax :
ְ߳
Tmax :
ְ߳ ð
t1/2 :
ҽ ݰ
* ġ αȯ ġ 90% ŷڱ
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. Ǿǰ 72 , Žü0.2и(Žνſ꿰)[()ٻ] Žü0.4и(Žνſ꿰)[()ٻ] ڷḦ
Ͽ, Ͽ. ̿
ش ڷμ Ͽ.
1. ()ٻ Žü0.4и(Žνſ꿰) Ḧ Ͽ ()ٻ Ź Ͽ.
12. Ÿ
1) ĵ
ӽ Ʈ 300 mg/kg/day(
ġ뷮 50) ڿ ϴٴ Ŵ Ÿ
ʾҴ. ӽ 䳢 50 mg/kg/day
ڿ ϴٴ Ŵ Ÿ ʾҴ.
2) ൿ
ǰ Žνſ꿰 0.2mg ĸ (Žν 0.4mg ĸ)
̿ Բ Ͽ , AUC Cmax
뷮 ʼ Ǿ.