TABLE 3

Fraction unbound in plasma and tissues, fraction un-ionized in blood (fuib) and tissues (fuit) (%) and blood-to-plasma concentration ratio (BP) in rats

CompoundfutfupfuibfuitBP
LungBrainHeartBoneMuscleAdiposeSkinThymusKidneyTestesLiverSpleenPancreasIntestine
%
Cefotetan3126232315251419242616241721413.4 × 10−92.1 × 10−80.9
Cefazolin3973782653392126565139734122131.6 × 10−34.0 × 10−30.5
Cefpiramide3341332420241121324823473639311.6 × 10−34.2 × 10−30.5
Cefoperazone4454514122332833274039423833361.6 × 10−34.2 × 10−31.1
Furosemide222013229.52114171025102118301.30.00430.0111.1
Diclofenac114.23.1164.4105.43.84.46.71.94.92.32.10.780.0600.150.6
Rosuvastatin916239802910067523551324836748.40.0710.180.7
Fluvastatin2.90.610.640.880.534.81.00.540.710.950.470.780.710.540.600.0740.191.0
Warfarin312216601731111521277.0186.07.91.40.130.320.6
Ethinylestradiol1.90.230.781.51.00.570.520.680.711.50.711.11.61.01.61001000.8
Cyclosporine2.71.21.13.61.30.570.170.170.400.130.810.230.610.232.91001000.7
TC14830266021251226241916104.04.4191001000.7
C22924196123231234222617168.717101001000.7
TC33722267022361738161514139.310271001000.6
Diazepam8.95.64.2115.51.01.32.75.56.42.85.70.882.8111001000.8
TC40.510.0400.0370.0970.0520.160.350.180.110.220.310.0730.540.100.26100990.7
TC51.41.10.883.01.10.240.200.711.20.920.510.470.230.741.8100990.6
Midazolam5.63.33.46.97.11.80.712.13.94.92.23.81.01.32.899960.9
TC69.55.66.51.26.16.65.21.14.34.82.14.21.01.40.3098950.6
TC71.60.810.810.131.40.700.360.270.811.30.471.20.611.00.1097920.4
TC89.55.66.51.26.16.65.21.14.34.82.14.21.01.40.7097920.5
Nicardipine1.80.540.710.571.70.490.830.710.851.00.510.920.740.641.456340.8
TC96.23.22.95.03.58.74.42.43.33.40.851.70.780.743.0198.51.1
Erythromycin575144424939255441474457118.548156.51.1
Lidocaine926360100941006810030655810058100386.92.91.3
Verapamil15137.3106.8141.58.29.18.72.8110.340.444.02.61.11.2
Propranolol7.84.13.65.66.16.21.34.54.54.91.75.52.30.888.81.80.721.2
Metoprolol6246464545462539543337451410801.70.671.0
Quinidine3.28.96.31.35.08.40.601.55.36.31.36.00.200.80171.30.521.1
Propafenone4.81.91.51.93.49.01.62.71.92.50.782.75.40.472.21.30.511.1
Irinotecan189.31210152512109.1115.7125.99.25.11.10.450.9
Imipramine3.83.52.24.03.52.20.682.22.92.31.12.71.00.57150.810.321.4
Citalopram129.27.3158.3201.9128.9124.0130.470.88400.670.271.2
Disopyramide3938383531281935454237493025610.200.0791.1
Naltrexone38404340355628425156385624254842232.1
Dasatinib2.51.20.881.21.23.41.30.881.21.60.470.810.370.302.087721.4