2005 1 872646 IF 1998 9 1g 3mg(0.3%) Deprodone Propionate 2003227 200374 1997415( ) 1998316( ) F A X 2003 7 1992 3 17 1997 10 9 1992 5 22 1997 12 19 IF 2005 4
IF 1. MR 63 2 IF 10 3 IF 2. IF IF IF 3. IF A4 9 IF IF IF 11 1 IF IF 4. IF IF MR IF IF MR Drug Safety Update IF
1985 3 1985 7 1988 1 1992 3 1987 1997 10 (1) (2) (3) 84.3%(721 /855 ) 96.3%(823 /855 ) 81.4%(664 /816 93.8%(765 /816 ) 78.5%(520 /662 92.6%(613 /662 ) (4) 1.0%(9 /859 ) 2.1%(17 /824 ) 1.6%(12 /728 ) - 1 -
0.3% 0.3% 0.3% ECLAR OINTMENT 0.3%, ECLAR CREAM 0.3%, ECLAR LOTION 0.3% JAN Deprodone Propionate INN C24H32O5 400.51 (+)-11,17-dihydroxy-1,4-pregnadiene-3,20-dione 17-propionate - 2 -
CAS 20424-00-4-3 -
225230 Britton-Robinson (ph210) ( / ) 0.0020.006 20 D α 23 27 0.4g 20mL100mm - 4 -
(1) 2mg 2mL 365nm 10mL (2) (1100)1mL 1mL 2 (3) 0.05g 2mL 5 272mL 1 (4) ( ) - 5 -
- 6 -
1g 3mg0.3 ph4.55.5 3 (200 ) 3 50m 0.5% ph4.04.8 1.000.05 HP2100-O( ) HP2101C( ) HP2102L( ) 1g 3mg0.3-7 -
1) - 8 -
1) 2) - 9 -
1) 0.7g( 2mg ) 10mL 10 30mL 10 1mL 1mL 2 2) 0.7g 10mL 10 30mL 10 1mL 0.02g 10mL 5L (60:15:10:3) 12cm 110 10 ( 365nm) Rf (0.3) 1) 0.7g( 2mg ) 30mL 30mL 2 1mL 1mL 2 2) 0.7g 30mL 30mL 2 1mL 0.02g 10mL 5L (60:15:10:3) 12cm 110 10 ( 365nm) Rf (0.3) 1) 0.7g( 2mg ) 20mL 2g 30mL 2 1mL 1mL 2-10 -
2) 0.7g 20mL 2g 30mL 2 1mL 0.02g 10mL 5L (60:15:10:3) 12cm 110 10 ( 365nm) Rf (0.3) 1)3) 0.7g( 2mg ) 20mL 2g 30mL 3 100mL 10mL 10mL 105 3 0.05g 100mL 2mL 50mL 10mL 10mL 20L QT QS (mg) (mg)qt/qs1/25 n- (120000) - 11 -
( ) ( ) ( ) 964 707 1671 662-12 -
- 13 -
DNA RNA DNA mrna mrna mrna 7)8) 30mg 15 1 2 1 2 (p<0.01) (p<0.01) - 14 -
15 2 2-15 -
DP-O Control DP-O 34 5 BV-O DP-O DP-C Control DP-C 34 5 BV-C DP-C ( ) 2 50mg 11) (mg) (%) (mg/100gb.w.) Control 8 50.44.0 154.25.0 DP-O 8 52.12.9 3.4 143.610.0 DP-O 8 34.32.9**,## 31.9 (34.2 a ) 115.58.1**,# BV-O 8 27.81.5** 44.8 071.64.2**,$$ - 16 - ( S.E.) DP-O 7 Control DP-O BV-O DP-O BV-O DP-O
(mg) (%) (mg/100gb.w.) Control 8 50.44.0 154.25.0 DP-C 8 51.12.3 01.4 130.58.1* DP-C 8 29.81.8**,## 40.9 (41.7 a ) 120.36.4** BV-C 8 29.32.4** 41.9 076.53.7**,$$ ( S.E.) DP-C 7 Control DP-C BV-C DP-C BV-C DP-C BV-O Control 3 (17 )7 (21 ) DP-O BV-O 3 (17 ) 7 (21 ) DP-O BV-O - 17 -
( ) 15 1 1 100mg - 18 -
1) 14) 5 2g( 6mg)12 EIA (DP) 12 6,11,17- -1,4- -3,20-17- (M2) 15 48 (4pg/mL) - 19 -
- 20 -
20 2g( 6mg) 12 6-12 6-15 48 6- (4pg/mL) 0.06% - 21 -
AUC0 1203.5230.1(pghr/mL) AUC0 1494.2496.9(pghr/mL) AUC0 1740.6810.0(pghr/mL) Kel0.1140.077(hr -1 ) Kel0.0920.023(hr -1 ) Kel0.0860.022(hr -1 ) 7880(%) - 22 -
CYP450 0.06% - 23 -
2-24 -
ODT 3,753 16 (0.43%) 4 (0.11%) 4 (0.11%) 4 (0.11%) 4 (0.11%) 2,119 34 (1.60%) 13 (0.61%) 7 (0.54%) 6 (0.28%) 5 (0.24%) 5 (0.24%) 728 12 (1.65) 6 (0.82%) 5 (0.69%) 4 (0.55%) ( ) ODT - 25 -
- 26 -
ODT (ODT) - 27 -
- 28 -
17) 2) ( ) 80mg/kg 18)19) 1) (SD 5 n=20 20) 0.04mg/kg/day15 2) ( n=3 3) 0.2mg/kg/day13 2mg/kg/day 3) ( n=2 2) 0.1mg/kg/day 1 5mg/kg/day 50mg/kg/day 2 18) 1) (SD 5 n=30 30) 0.010.040.6mg/kg/day 52 (4 ) 0.04mg/kg/day 0.01mg/kg/day 2) ( n=6 6) 12 0.04mg/kg/day 0.01mg/kg/day 0.01mg/kg/day - 29 -
SD 6 (n=20) 60 (n=20) 14 7 0.01mg/kg/day 0.08mg/kg/day 0.6mg/kg/day 0.6mg/kg/day 0.08mg/kg/day 0.08mg/kg/day 0.01mg/kg/day (SD 10 n=30) 7 11 0.4mg/kg/day 0.08mg/kg/day 10mg/kg/day 0.08mg/kg/day ( n=12) 13 0.08mg/kg/day 2mg/kg/day 0.4mg/kg/day 0.08mg/kg/day (SD 10 n=25) 17 21 2628 0.6mg/kg/day 0.01mg/kg/day 0.08mg/kg/day 0.08mg/kg/day 0.6mg/kg/day 24) (Hartley n=5) ASA PCA 24) (Hartley ) 24) (Hartley ) Maximization - 30 -
25) 3H- 96 240 AUC0 720 4.3 3H- 24 144 2 AUC0 720 4.7 3H- (0.1mg/kg) 1 120 3H- (0.4mg/kg) - 31 -
(SD ) 3H- (0.6mg/kg) 168 2.5% 8.6% 11.2% 12% (SD ) 3H- (0.6mg/kg) 168 2.9% 10.5% 13.3% 14% 18 3H- 24 ( 0.4mg/kg) - 32 -
3 3 3 5g105g5010g10 500g 5g105g5010g10 10g1010g50-33 -
2003 2 27 1992 327 2003 2 27 1997 10 9 4AM 760 4AM 761 20900AMZ00600000 2003 7 4 1992 522 2003 7 4 1997 12 19 2646729M1048 2646729N1031 2646729Q1031-34 -
1) ( ) 2) ( ) 3) ( ) 4) ( ) 5) 0.3%Deprodone Propionate (DP ) 5(9)159,1989 6) DP ( ) 7) 67(10)1935,1985 8) Therapeutic Research5(6)955,1986 9) ( ) 10) DP DP ( ) 11) Deprodone Propionate(DP) ( ) 23(15)93,1989 12) DP-L( ) ( ) 13) Deprodone propionate ( ) 14) ( ) 15) Deprodone propionate(dp) ( ) 16) ( ) 17) DP ( ) 18) ( ) 19) Deprodone Propionate(DP) 15 5 24(6)7,1990 20) Deprodone Propionate(DP) 24(6)25,1990 21) Deprodone Propionate(DP) 24(6)37,1990 22) Deprodone Propionate(DP) 24(6)59,1990 23) ( ) 24) Deprodone Propionate(DP) ( ) 23(15)7,1989-35 -
25) ( ) 26) ( ) 27) Deprodone Propionate ( ) 23(15)103,1989 28) ( ) 29) ( ) 30) ( ) - 36 -
- 37 -
- 38 -
MKI10506G ECL DB003A