TABLE 5.
Pharmacokinetic parameters of CEP in different dosages and route of administration in humans.
| N.O. | Drug | Usage | Dosage (mg) | Pharmacokinetic parameters | Bioavailability (F %) | Sample size | Detection method and LLOQ | References | |
|---|---|---|---|---|---|---|---|---|---|
| A | CEP | p.o., single treatment | 10 | Cmax (ng/mL) | 0.53 ± 0.06 | — | n = 2 | HPLC | Kohtaro et al. (1989), Moro et al. (1989) |
| Tmax (h) | 2.5 ± 0.5 1 | ||||||||
| t1/2 (h) | 4.1 ± 0.1 | ||||||||
| AUC(0–t) (ng/mL·h) | 2.78 ± 0.13 | ||||||||
| AUC(0–∞) (ng/mL·h) | 3.49 ± 0.09 | ||||||||
| CL (L/h) | - | ||||||||
| B | 30 | Cmax (ng/mL) | 2.35 ± 0.48 | — | n = 5 | ||||
| Tmax (h) | 1 ± 0.2 | ||||||||
| t1/2 (h) | 9.2 ± 1.3 | ||||||||
| AUC(0–t) (ng/mL·h) | 18.6 ± 4.5 | ||||||||
| AUC(0–∞) (ng/mL·h) | 23.8 ± 6.1 | ||||||||
| CL (L/h) | 1,792 ± 574 | ||||||||
| C | 60 | Cmax (ng/mL) | 3.46 ± 0.27 | — | n = 5 | ||||
| Tmax (h) | 1.1 ± 0.2 | ||||||||
| t1/2 (h) | 6.8 ± 0.5 | ||||||||
| AUC(0–t) (ng/mL·h) | 27.4 ± 3.2 | ||||||||
| AUC(0–∞) (ng/mL·h) | 26.4 ± 2.8 | ||||||||
| CL (L/h) | 2,390 ± 285 | ||||||||
| D | 120 | Cmax (ng/mL) | 6.78 ± 1.11 | — | n = 5 | ||||
| Tmax (h) | 1.2 ± 0.3 | ||||||||
| t1/2 (h) | t1/2a: 3.3 ± 1.0 t1/2β: 17.1 ± 4.1 | ||||||||
| AUC(0–t) (ng/mL·h) | 65.9 ± 7.4 | ||||||||
| AUC(0–∞) (ng/mL·h) | 131.3 ± 28.5 | ||||||||
| CL (L/h) | 1,094 ± 228 | ||||||||
| E | i.v., single treatment in 5 min | 25 | Cmax (ng/mL) | 187 ± 14 | 9 | n = 5 | HPLC | ||
| t1/2 (h) | 35.8 ± 3.2 | ||||||||
| AUC(0–48 h) (ng/mL⋅h) | 110.4 ± 92 | ||||||||
| AUC(0–∞) (ng/mL·h) | 158.8 ± 15.8 | ||||||||
| CL (L/h) | 164 ± 18 | ||||||||
| F | CEP | i.v., single treatment in 5 min | 50 | Cmax (ng/mL) | 433 ± 25 | 6 | n = 5 | ||
| t1/2 (h) | 36.9 ± 3.6 | ||||||||
| AUC(0–48 h) (ng/mL⋅h) | 252.9 ± 14.8 | ||||||||
| AUC(0–∞) (ng/mL·h) | 377.8 ± 22.7 | ||||||||
| CL(L/h) | 136 ± 17 | ||||||||
| G | CEP | i.v., single treatment in 5 min | 100 | Cmax (ng/mL) | 1,464 ± 364 | 9 | n = 5 | ||
| t1/2 (h) | 31.8 ± 0.8 | ||||||||
| AUC(0–48 h) (ng/mL⋅h) | 730.5 ± 86.2 | ||||||||
| AUC(0–∞) (ng/mL·h) | 962.5 ± 101.6 | ||||||||
| CL(L/h) | 102 ± 8 | ||||||||
| H | CEP | i.v., treatment in 5 min, continuously for 7 days | 100 | Cmax (ng/mL) | 196.3 ± 27.50 | — | n = 5 | ||
| Cmin (ng/mL) | 34.0 ± 2.32 | ||||||||
| t1/2 (h) | 62.0 ± 2.8 | ||||||||
| I | CEP | i.v., single treatment in 60 min | 50 | Cmax (ng/mL) | 135.9 ± 66.9 | — | n = 12 | HPLC-MS/MS;0.1 ng/mL | Hao et al. (2010) |
| Tmax(h) | 0.75 ± 0.21 | ||||||||
| t1/2 (h) | 131.9 ± 48.4 | ||||||||
| AUC(0–192 h) (ng/mL·h) | 566.6 ± 216.6 | ||||||||