TABLE 1.
Pharmacokinetic profile of IDV in combination with RTV taken with a low-fat meal after 2 weeks of dosing and with a high-fat meal on day 15a
| Dose | n |
Cmax (mg/liter)
|
AUC24 (estimateda) (mg · h/liter)
|
Ctrough (mg/liter)d
|
|||
|---|---|---|---|---|---|---|---|
| Low fat | High fat | Low fat | High fat | Low fat | High fat | ||
| IDV-RTV, q12h | |||||||
| 800-100 mg | 10 | 11.7 (10.4, 13.1) [9.6 to 15.2] | 9.6 (8.2, 11.2) [6.2 to 14.8] | 142.5c (120.4, 168.6) [112.8 to 239.4] | 119.7c (97.3, 147.2) [77.4 to 244.7] | 1.396 (0.979, 1.991) [0.816 to 4.701] | 1.371 (0.923, 2.037) [0.578 to 5.934] |
| 800-200 mg | 8 | 12.9 (11.4, 14.6) [8.5 to 16.1] | 11.6 (9.6, 13.9) [7.0 to 17.9] | 187.5c (156.6 224.5) [114.8 to 263.3] | 173.8c (136.9, 220.6) [80.5 to 299.5] | 3.119 (2.133, 4.559) [1.019 to 6.039] | 3.281 (2.076, 5.182) [0.919 to 6.791] |
| 800-400 mg | 9 | 10.9 (9.6, 12.4) [8.4 to 13.8] | 10.3 (8.7, 12.2) [8.6 to 13.4] | 163.6c (139.5, 195.9) [112.5 to 263.4] | 161.6c(129.6, 201.6) [126.5 to 217.3] | 3.105 (2.124, 4.538) [1.754 to 8.687] | 3.392 (2.222, 5.179) [1.321 to 5.536] |
| 400-400 mg | 10 | 7.0 (6.2, 7.9) [5.3 to 11.7] | 5.4 (4.6, 6.3) [3.4 to 7.9] | 85.8 (72.5, 101.5) [50.6 to 131.2] | 74.0 (60.2, 90.9) [38.6 to 113.3] | 1.308 (0.917, 1.865) [0.334 to 3.390] | 1.161 (0.782, 1.725) [0.315 to 2.874] |
| 800 mg of IDV q8h Merck 021, without food; Day 15 as monotherapy | 16 | 7.3 (6.3, 8.6) [3.4 to 12.6] | 52.9 (44.6, 62.7) [21.8 to 91.6] | 0.127 (0.098, 0.168) [0.047 to 0.446] | |||
a
Statistical significance testing was performed for AUC only. Data shown are ANOVA model-based geometric means (95% confidence intervals) [range]. Historical data for 800 of IDV q8h without food is provided for comparison.
b
AUC0–τ × doses/day.
c
Data were significantly different from data of the IDV-RTV 400-400 mg regimen at P values of 0.004 (low-fat meal) and <0.005 (high-fat meal).
d
Data used were C12 for IDV-RTV regimens and C8 for historical data for 800 mg of IDV q8h alone.