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. 2020 Mar 12;15(3):e0230195. doi: 10.1371/journal.pone.0230195

Table 2. Tacrolimus pharmacokinetics parameters in whole blood and PBMC (n = 32).

Median [range] Mean (SD)
Dose (mg/12 h) 1.5 [0.5–4] 1.8 (1.0)
Dose (mg/kg/12h) 0.017 [0.005–0.048] 0.021 (0.012)
Whole blood pharmacokinetics (WB)
Cmax (ng/mL) 17.7 [3.5–36.3] 16.4 (6.9)
Cmax/dose (ng/mL/mg) 9.5 [3.0–21.4] 10.8 (5.2)
Tmax (h) 1.6 [0.2–6] 1.9 (1.4)
C0 (ng/mL)a 6.2 [2.5–10.0] 6.4 (2.2)
C0/dose (ng/mL/mg) 3.9[1.1–17.7] 5.1 (4.2)
AUC0–12h (ng∙h/mL) 102.3 [35.0–215.5] 108.9 (38.9)
Cl/F (L.h-1) 16.2 [5.0–39.2] 17.8 (9.0)
Intracellular pharmacokinetics (PBMC)
Cmax (pg/million PBMC) 71.3 [25.7–156.0] 78.1 (37.1)
Cmax/dose (pg/million PBMC/mg) 44.2[17.1–258.7] 56.1 (46.1)
Tmax (h) 1.6 [0.3–6] 1.9 (1.2)
C0 (pg/million PBMC) 28.4 [9.6–80.4] 37.2 (17.7)
C0/dose (pg/million PBMC/mg) 20.0 [3.2–67.2] 24.8 (16.8)
AUC0–12h (pg∙h/million PBMC) 491.6 [223.0–1127.2]
Whole blood—intracellular relationships
Intracellular diffusion ratio
(AUC0–12h PBMC / AUC0–12h WB)
23.6 [14.8–39.7] 24.9 (6.9)
r2 (p)
Correlation AUC0–12h PBMC & AUC0–12h WB 0.51 (<0.001)
Correlation C0PBMC & C0WB 0.39 (<0.001)
Correlation CmaxPBMC & CmaxWB 0.53 (<0.001)
Correlation CmaxPBMC & C0WB 0.17 (0.02)
Correlation AUC0–12h PBMC & C0WB 0.53 (<0.001)

Cmax: maximum concentration; Tmax: time when Cmax is achieved; C0: predose concentration; AUC0-12h: area under the concentration–time curve from 0h to 12h; Cl/F: apparent clearance; PBMC: peripheral blood mononuclear cells; WB: whole blood; SD: standard deviation; r2: coefficient of determination; p: p-value

a: the day of the study, 81.2% of patients had tacrolimus whole blood concentration between 4–10 ng/mL.