Table 1.
Key pharmacokinetic parameters for plasma, subcutaneous adipose tissue, and cancellous and cortical bone. Values are medians (95% CI) unless otherwise stated.
| Pharmacokinetic parameter |
Plasma (unbound) |
Subcutaneous adipose tissue |
Cancellous bone |
Cortical bone |
Overall comparisona |
|---|---|---|---|---|---|
| AUC0–last (min µg/mL) | 6,296 (5,883–6,709) | 1,545 (698–2,392)c | 2,636 (1,527–3,744)c | 1,016 (661–1371)c,d | < 0.001 |
| Cmax (µg/mL)b | 34.3 (31.3–37.2) | 6.6 (3.4–9.8)c | 10.8 (6.3–15.3)c | 4.0 (2.5–5.4)c,d | < 0.001 |
| Tmax (min) | 100 (64–136) | 200 (120–281) | 148 (73–223) | 152 (81–223) | – |
| T1/2 (min) | 362 (311–414) | 583 (8–1,158) | 360 (21–700) | 392 (67–716) | 0.8 |
| AUCtissue/AUCplasma | 0.31 (0.16–0.46) | 0.45 (0.29–0.62) | 0.17 (0.11–0.24) | 0.008e |
AUC0–last = area under the concentration-time curve from 0 to the last measured value;
Cmax = peak drug concentration; Tmax = time to Cmax; T1/2 = half-life at β-phase;
AUCtissue/AUCplasma = tissue penetration expressed as the ratio of AUCtissue/AUCplasma
a
Overall comparison using Wald’s test for free plasma, subcutaneous adipose tissue, cancellous, and cortical bone.
b
Values are means (95% CI).
c
p < 0.001 for comparison with the corresponding free plasma value.
d
p < 0.007 for comparison with cancellous bone.
e
T-test comparison of cancellous and cortical bone.