Table 2.
Pharmacokinetic Parameters of IV- or SC-Delivered FAF–Rapa Analyzed Using Compartmental Analysis and Noncompartmental Analysis (Mean ± SD)
| route of administration | ||||
|---|---|---|---|---|
| parameter (unit) | IV | SC | IV | SC |
| preferred model | one compartment | three compartments | noncompartment | |
| AUC (μM·hr) | 141 ± 16 | 92 ± 19 | 207 ± 33 | 109 ± 14 |
| AUMC (μM·hr2) | - | - | 2207 ± 344 | 2214 ± 328 |
| F (%) | 100 | 65.5 ± 13.2 | 100 | 52.7 ± 6.7 |
| CL (mL/h) | 0.15 ± 0.01 | 0.15a | 0.10 ± 0.01 | 0.09 ± 0.01 |
| CL/F (mL/h) | 0.15 ± 0.01 | 0.23 ± 0.04 | 0.10 ± 0.01 | 0.18 ± 0.03 |
| Vd (mL) | 1.46 ± 0.2 | 1.46a | 0.88 ± 0.1 | 0.85 ± 0.1 |
| Cmax (μM) | 13.4 ± 2.4 | 3.3 ± 0.1 | 11.7 ± 2.9 | 4.4 ± 0.7 |
| Tmax (hr) | 0.0 | 12.4 ± 0.7 | 0.0 | 12.0 |
| MRT (hr) | - | - | 10.7 ± 0.3 | 20.3 ± 1.1 |
| MAT (hr) | - | - | - | 9.6 ± 1.1 |
| Tl/2,absorption (hr) | - | 4.2 ± 0.4 | - | - |
| Tl/2,elimination (hr) | 6.9 ± 0.5 | 6.9a | 6.2 ± 0.4 | 6.4 ± 0.7 |
| kabsorption (hr−1) | - | 0.16b | - | - |
| kelimination (hr−1) | 0.10 ± 0.01 | 0.10a | 0.11 ± 0.01 | 0.11 ± 0.01 |
| kdegradation (hr−1) | - | 0.09 ± 0.05 | - | - |
a
Compartmental values from IV analysis were adopted to estimate other SC parameters.
b
To fit the observed time to peak concentration, the assumption was required that kabsorption = kinjection site→interstitial = kinterstitial fluid→systemic circulation.