Pharmacokinetic parameters of 12 drugs in female SD rats
Female SD rats received a bolus intravenous injection of 0.2 mg/kg pitavastatin, 0.5 mg/kg rosuvastatin, 0.5 mg/kg valsartan, 0.08 mg/kg olmesartan, 0.08 mg/kg candesartan, 0.5 mg/kg temocaprilat, 0.5 mg/kg enalaprilat, 0.5 mg/kg benazeprilat, 2 mg/kg PCG, and 1 mg/kg ceftizoxime or constant infusion of pravastatin (76 mg/min/kg after intravenous administration of 0.67 mg/kg) and cefmetazole (0.1 mg/min/kg). The concentrations of drugs in plasma, bile, and urine were measured, and pharmacokinetic parameters were calculated. Each value is expressed as mean ± S.E. of four to five rats. No. for each compound corresponds to the numerical coding attached to each plot in all the figures.
No. | Compound | CLtot, B | CLbile, B | CLrenal, B | fbile | furine | |
|---|---|---|---|---|---|---|---|
| ml/min/kg | % of dose | ||||||
| 1 | Pravastatin | 123 ± 15 | 78.3 ± 6.0 | 32.5 ± 5.2 | 65.8 ± 4.8 | 26.0 ± 1.6 | |
| 2 | Pitavastatin | 17.8 ± 2.4 | 12.2 ± 1.7 | 0.0108 ± 0.0011 | 63.8 ± 2.3 | 0.0564 ± 0.0236 | |
| 3 | Rosuvastatin | 127 ± 7 | 111 ± 5 | 8.42 ± 2.09 | 83.9 ± 2.5 | 6.34 ± 1.61 | |
| 4 | Valsartan | 22.3 ± 1.3 | 16.0 ± 0.7 | 0.405 ± 0.171 | 81.5 ± 2.9 | 1.86 ± 1.39 | |
| 5 | Olmesartan | 3.83 ± 0.47 | 2.99 ± 0.45 | 0.0238 ± 0.0023 | 86.8 ± 3.4 | 0.587 ± 0.090 | |
| 6 | Candesartan | 4.14 ± 0.23 | 3.03 ± 0.24 | 0.200 ± 0.019 | 73.6 ± 3.1 | 4.94 ± 0.58 | |
| 7 | Temocaprilat | 53.0 ± 1.0 | 34.4 ± 2.6 | 7.81 ± 1.04 | 72.7 ± 4.2 | 16.5 ± 2.1 | |
| 8 | Enalaprilat | 22.8 ± 2.5 | 2.96 ± 0.32 | 17.4 ± 2.1 | 13.4 ± 0.1 | 76.1 ± 3.4 | |
| 9 | Benazeprilat | 46.1 ± 3.5 | 20.2 ± 2.9 | 24.0 ± 0.8 | 43.7 ± 6.6 | 53.0 ± 4.8 | |
| 10 | PCG | 62.4 ± 1.7 | 8.66 ± 1.10 | 42.6 ± 1.3 | 14.4 ± 1.8 | 71.1 ± 2.6 | |
| 11 | Ceftizoxime | 23.3 ± 2.9 | 1.21 ± 0.16 | 19.5 ± 1.8 | 5.32 ± 0.18 | 86.2 ± 3.5 | |
| 12 | Cefmetazole | 54.3 ± 5.2 | 24.2 ± 2.1 | 24.0 ± 1.4 | 46.7 ± 8.1 | 45.5 ± 5.7 | |