Table 3.
Physicochemical, physiological and pharmacokinetic input parameters used for the development of PBPK model of ciprofloxacin using GastroPlusTM.
| Input parameter | Value | Source |
|---|---|---|
| Log P | 1.7 | Olivera et al.36 |
| pKa | 6.2/8.59 | Olivera et al.36 |
| Molecular weight (MW) (g/mol) | 385.8 | Balbas-Martinez et al.30 |
| Aqueous solubility (S) (mg/ml) | 10 to 30 | Olivera et al.36 |
| Jejunal effective permeability (Peff) (cm/sec × 10–4) | 0.29 | Wang et al.28 |
| Unbound percent in human plasma (% Fup) | 0.60–0.80 | Wingender et al.32 |
| Human blood to plasma concentration ratio (Rbp) | 1.25 | ADMET Predictor™ |
| Cl total (l/h/kg) | 0.34 | Gonzalez et al.34 |
| Cl Renal (l/h) | 22 | Höffken et al.31 |
| Cl biliary (ml/min/kg) | 1.25 | Lettieri et al.33 |
| T1/2 (h) | 4.78 | PKPlus™ |
| K12 (1/h) | 2.11 | PKPlus™ |
| K21 (1/h) | 1.598 | PKPlus™ |
| Vss (l/kg) | 1.74–5 | Vance-Bryan et al.35 |
| Vd (l/kg) | 1.1 | Montgomery et al.29 |