Table 1.
Pharmacokinetic parameters of unbound cefadroxil in rat blood and brain on Day 1 (Control, Ctrl) and Day 2 (with probenecid, Pro)
| Parameters | Unit | Day 1 (Ctrl) | Day 2 (Pro) | Pro/Ctrl |
|---|---|---|---|---|
| Blood | ||||
| AUCu (0–420) | μg*min/mL | 1747 ± 90 | 2801 ± 175*** | 1.60 |
| AUCu (0-inf) | μg*min/mL | 1802 ± 97 | 2873 ± 177*** | 1.59 |
| Cu,ss,blood | μg/mL | 8.5 ± 0.4 | 13.8 ± 0.9*** | 1.62 |
| MRTiv | min | 71 ± 4 | 77 ± 4 | 1.05 |
| t1/2 | min | 49 ± 2 | 53 ± 3 | 1.09 |
| CL | mL/min/kg | 16.9 ± 1.0 | 10.7 ± 0.7*** | 0.63 |
| Vss | L/kg | 1.19 ± 0.12 | 0.82 ± 0.10*** | 0.69 |
| Brain ECF | ||||
| AUCu (0–420) | μg*min/mL | 31 ± 5 | 122 ± 31* | 3.93 |
| AUCu (0-inf) | μg*min/mL | 40 ± 7 | 174 ± 35** | 4.37 |
| Kp,uu,ECF (0–420) | 0.018 ± 0.003 | 0.042 ± 0.009* | 2.35 | |
| Kp,uu,ECF (0-inf) | 0.022 ± 0.003 | 0.058 ± 0.009* | 2.63 | |
| Brain CSF | ||||
| AUCu (0–420) | μg*min/mL | 39 ± 12 | 73 ± 27 | 1.88 |
| AUCu (0-inf) | μg*min/mL | 57 ± 15 | 117 ± 50 | 2.04 |
| Kp,uu,CSF (0–420) | 0.022 ± 0.006 | 0.024 ± 0.008 | 1.13 | |
| Kp,uu,CSF (0-inf) | 0.031 ± 0.007 | 0.039 ± 0.015 | 1.26 |
Data are expressed as mean ± SEM (n = 6). A paired t-test was performed to compare cefadroxil parameters between the control (without probenecid) and treatment (with probenecid) phases of the study. *p < 0.05, **p < 0.01, and ***p < 0.001. Abbreviations: AUC u, Area under the unbound concentration-time curve from time zero to 420 min (0–420) or from time zero to infinity (0-inf); C u,ss,blood, Unbound steady-state blood concentration; MRT iv, Mean residence time; t1/2, Half-life; CL, Total clearance; V ss, Volume of distribution steady-state; K p,uu,ECF, Ratio of AUCu in brain ECF to AUCu in blood; and K p,uu,CSF, Ratio of AUCu in CSF to AUCu in blood.