TABLE 2

Clearance obtained for 10 drugs in the presence and absence of BSA using combined P450 and UGT cofactors and scaled to in vivo


Compound

CLint, u (P450 + UGT)

-Fold Difference: Clint, u + BSA/CLint, u - BSA

fumic

Scaled CLint, ua
-BSA
+BSA
-BSA
+BSA
-BSA
+BSA
μl/min/mg ml/min/kg
Buprenorphine 688 577 0.84 0.10 0.17 588.9 494
Carvedilol 356 246 0.69 0.10 0.04 305 210
Codeine 3.4 16.9 5.0 0.96 0.99 2.9 14.5
Diclofenac 369 2143 5.8 0.87 0.008 316 1834
Gemfibrozil 97.3 1274 13.0 0.77 0.01 83.3 1090
Ketoprofen 26.0 115 4.4 0.92 0.11 22.2 98.5
Midazolam 159 241 1.5 0.54 0.04 137 207
Naloxone 14.4 35.1 2.4 0.87 0.99 12.3 30.1
Raloxifene 544 1812 3.3 0.08 0.009 465 1551
Zidovudine
2.8
13.2
4.7
0.60
0.49
2.4
11.3