Table 2.
Pharmacokinetic parameters of ciclosporin in subjects treated with CicloMulsion® or Sandimmune® as a single intravenous infusion over 4 h at a dose of 5 mg/kg
| Parameter (unit) | CicloMulsion® (n = 52) | Sandimmune® injection (n = 52) | ||||
|---|---|---|---|---|---|---|
| Mean | SD | CV (%) | Mean | SD | CV (%) | |
| Cmax (ng/mL) | 2,972 | 381 | 12.8 | 3,134 | 386 | 12.3 |
| AUC0–last (ng ⋅ h/mL) | 19,412 | 3,202 | 16.5 | 21,679 | 4,165 | 19.2 |
| AUC0–∞ (ng ⋅ h/mL) | 20,519 | 3,488 | 17.0 | 22,904 | 4,466 | 19.5 |
| AUC4–∞ (ng ⋅ h/mL) | 11,496 | 2,569 | 22.3 | 13,349 | 3,626 | 27.2 |
| AUC0–4 (ng ⋅ h/mL) | 9,023 | 1,232 | 13.7 | 9,555 | 1,148 | 12.0 |
| AUC4–last (ng ⋅ h/mL) | 10,389 | 2,240 | 21.6 | 12,124 | 3,256 | 26.9 |
| CL (mL/h) | 17,446 | 2,543 | 14.6 | 15,746 | 2,860 | 18.2 |
| MRT (h) | 8.8 | 3.2 | 36.1 | 9.1 | 5.8 | 63.5 |
| t½β (h) | 14.6 | 6.4 | 43.4 | 14.7 | 8.2 | 55.7 |
| AUC extrapolation (%)a | 5.3 | 2.5 | 46.6 | 5.2 | 4.0 | 76.7 |
| tmax (h) | 3.7 | 0.4 | 11.4 | 3.7 | 0.4 | 10.1 |
AUC area under the blood concentration–time curve, CL clearance, C max maximum blood concentration, CV (interindividual) coefficient of variation, MRT mean residence time, SD standard deviation, t ½β apparent terminal half-life, tmax time to reach Cmax
aAUC extrapolation is the percentage of AUC0–∞ extrapolated from AUC0–last