Table VII.
Species | Drug μM | fu mean or range | Reference, meeting or website | |
---|---|---|---|---|
Propranolol | Warfarin | |||
Mouse | 1 | 0.10–0.11 | (117) | |
10 | 0.17 | 0.07 | a | |
10 | 0.15 | 0.06 | b | |
Rat | h | 0.010–0.018 | (117) | |
0.04 | 0.08 | (118) | ||
1 | 0.21 | 0.005 | c | |
1 | 0.003–0.004 | d | ||
1 | 0.28 | 0.005 | (119) | |
5 | 0.06 | e | ||
10 | 0.19 | 0.01 | a | |
10 | 0.15 | 0.007 | b | |
Rabbit | h | 0.042–0.052 | (117) | |
0.04 | 0.35 | (118) | ||
0.22–2.5 | 0.34 | (120) | ||
Dog | h | 0.040 | (117) | |
0.04 | 0.10 | (118) | ||
1 | 0.27 | 0.038 | c | |
1 | 0.20 | 0.033 | (119) | |
10 | 0.23 | 0.04 | a | |
10 | 0.20 | 0.046 | b | |
Guinea pig | 10 | 0.17 | 0.02 | a |
Minipig | 10 | 0.18 | 0.03 | a |
Monkey | 1 | 0.21 | (121) | |
1 | 0.21 | 0.005 | (119) | |
10 | 0.20 | 0.01 | c | |
Human | h | 0.012–0.022 | (117) | |
0.04 | 0.10 | (118) | ||
hi | 0.10 | f | ||
hi | 0.01 | g | ||
1 | 0.21 | 0.006 | (119) | |
1 | 0.14 | (121) | ||
1 | 0.13 | 0.011 | c | |
1 | 0.16 | 0.005–0.006 | d | |
1 | 0.29 | (122) | ||
1 | 0.13 | (123) | ||
1-3i | 0.005 | (124) | ||
5 | 0.27 | e | ||
10 | 0.12 | <0.01 | a | |
10 | 0.19 | 0.007 | b |
aBD Biosciences brochure (now Corning), In vitro ADME discovery screening services, plasma protein binding using rapid equilibrium dialysis
bBD Biosciences (now Corning) Application Note 474, 2009, Shanler M, Mason A, Crocker R, Vardaro R, Crespi C, Stresser D, Validation of an automated high throughput plasma protein binding assay
cwww.noabbiodiscoveries.com website
dPierce Biotechnololgy, Inc., www.piercenet.com, Li S, Xiong B, Huang T, Li L, Donovan J, Lee F, Yu S, Miwa G, and Yang H, Validation of a novel rapid equilibrium dialysis (RED) device for high throughput plasma protein binding determination, 2006
eWaters Corporation Application Note 720002610, Shave D and Alden P, Determination of protein binding by UPLC/MS/MS
fWyeth Package Insert, 2912389
gBristol-Myers Squibb Package Insert, 3022954
hdrug concentration not indicated
iValues reported from ex vivo plasma samples