TABLE 2.
Main PK parameters calculated for the study populationa
| Population and compartment | AUC0-8 for tissue/ AUC0-8 for free plasma | AUC0-8 (mg · h/liter) | AUC0-24b (mg · h/liter) | Cmax (mg/liter) | Tmax (h) | t1/2β (h) | CL (liters/h) | Vss (liters) |
|---|---|---|---|---|---|---|---|---|
| Entire population (n = 11) | ||||||||
| Plasma, total | 16.4 ± 5.5 | 29.5 ± 12.0 | 4.0 ± 1.1 | 1.0 ± 0.0 | 11.0 ± 3.1 | 13.0 ± 5.8 | 150 ± 42 | |
| Inflamed tissue | 0.9 ± 0.7 | 6.4 ± 4.1 | 9.7 ± 6.1 | 1.6 ± 1.2 | 2.1 ± 2.0 | 4.7 ± 1.3 | NDc | ND |
| Healthy tissue | 0.7 ± 0.5 | 5.9 ± 5.7 | 13.2 ± 16.4 | 1.2 ± 1.0 | 1.5 ± 0.8 | 6.3 ± 2.3 | ND | ND |
| Diabetic patients (n = 5) | ||||||||
| Plasma, total | 17.5 ± 5.4 | 33.6 ± 16.4 | 3.8 ± 1.0 | 1.0 ± 0.0 | 13.0 ± 3.5 | 10.9 ± 6.0 | 146 ± 48 | |
| Inflamed tissue | 0.5 ± 0.4 | 3.7 ± 1.9 | 6.0 ± 2.9 | 0.8 ± 0.5 | 2.8 ± 2.6 | 5.6 ± 1.1 | ND | ND |
| Healthy tissue | 0.9 ± 0.6 | 8.1 ± 7.1 | 20.8 ± 22.0 | 1.4 ± 1.1 | 1.8 ± 0.7 | 7.6 ± 2.2 | ND | ND |
| Nondiabetic patients (n = 6) | ||||||||
| Plasma, total | 15.4 ± 5.9 | 26.0 ± 10.6 | 4.1 ± 1.2 | 1.0 ± 0.0 | 8.6 ± 1.6 | 14.8 ± 5.6 | 152 ± 41 | |
| Inflamed tissue | 1.2 ± 0.8 | 8.7 ± 4.1 | 12.8 ± 6.4 | 2.3 ± 1.2 | 1.6 ± 1.3 | 4.1 ± 1.3 | ND | ND |
| Healthy tissue | 0.5 ± 0.3 | 4.1 ± 4.2 | 6.9 ± 7.1 | 1.0 ± 1.0 | 1.3 ± 0.8 | 5.2 ± 1.7 | ND | ND |
a
Data are means ± SDs for 11 patients.
b
Data for AUC for tissue were calculated from time zero to infinity.
c
ND, not determined.