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Table 1 Pharmacokinetic parameters of unbound cefadroxil in rat blood and brain on Day 1 (Control, Ctrl) and Day 2 (with probenecid, Pro)

From: Effect of transporter inhibition on the distribution of cefadroxil in rat brain

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
  1. 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.