TABLE 1

Plasma and tissue concentrations and tissue/plasma concentration ratios of atorvastatin after a 3.0 mg/kg s.c. administration to mdr1a/b KO and WT mice

Concentration in plasma, liver, and brain at 0, 0.5, 1.5, and 3 h postdose that are not shown in the table were below the lower limit of quantitation (acid/lactone): 5/10 ng/ml in plasma, 5/5 ng/ml in brain homogenate, and 10/10 ng/ml in liver homogenate. Data are means ± S.D.

Form Dosed
Form Measured
Matrix
Time
KO
WT
Conc.
Tissue/Plasma Ratio
Conc.
Tissue/Plasma Ratio
h ng/ml ng/ml
Lactone Lactone Plasma 0.5 12 ± 3 13 ± 3
Acid Plasma 0.5 23 ± 4 28 ± 6
Acid Acid Plasma 0.5 593 ± 248 543 ± 79
Plasma 1.5 112 ± 35 145 ± 30
Plasma 3 37 ± 16 91 ± 27
Liver 0.5 1113 ± 169 2.1 ± 0.9 915 ± 247 1.7 ± 0.3
Liver 1.5 360 ± 168 3.5 ± 1.8 340 ± 20 2.4 ± 0.6
Liver 3 119 ± 64 3.2 ± 0.5 145 ± 64 1.6 ± 0.3
Brain
0.5
39 ± 5
0.074 ± 0.027
26 ± 1
0.044 ± 0.003