Table 2.
Raltegravir Pharmacokinetic Parameters by Cohort and Formulation
| Cohort | Descriptor | Dose, mg | Weight, kg | Dose, mg/kg | T1/2, h | Cmax, ng/mL | C12, ng/mL | AUC12, h*mg/L | CL/F, L/h | V/F, L |
|---|---|---|---|---|---|---|---|---|---|---|
| Cohort I (n = 11) | Mean | 390.9 | 43.5 | 9.3 | 4.9 | 2813.1 | 197.0 | 10.2 | 71.7 | 698.6 |
| ≥12 to <19 y | SD | 94.4 | 13.4 | 1.6 | 3.6 | 2673.9 | 154.2 | 10.0 | 56.7 | 1131.5 |
| Film-coated tablet | Median | 440.0 | 39.8 | 9.9 | 3.8 | 1384.1 | 137.6 | 7.4 | 54.1 | 223.6 |
| CV% | 24.1 | 30.8 | 17.3 | 73.9 | 95.1 | 78.3 | 97.6 | 79.1 | 162.0 | |
| GM | 379.6 | 45.1 | 9.1 | 5.0 | 1777.2 | 147.8 | 7.0 | 54.4 | 310.0 | |
| Cohort IIA (n = 11) | Mean | 400.0 | 31.5 | 13.4 | 3.7 | 4055.7 | 399.4 | 13.4 | 112.8 | 475.6 |
| ≥6 to <12 y | SD | 0.0 | 7.3 | 3.7 | 1.4 | 5269.5 | 880.9 | 16.1 | 161.4 | 506.7 |
| Film-coated tablet | Median | 400.0 | 32.4 | 12.3 | 3.4 | 2247.2 | 107.5 | 6.7 | 59.4 | 292.3 |
| CV% | 0.0 | 23.2 | 27.4 | 36.7 | 129.9 | 220.5 | 120.4 | 143.2 | 106.5 | |
| GM | 400.0 | 30.7 | 13.0 | 3.5 | 2135.0 | 109.4 | 7.0 | 56.8 | 287.9 | |
| Cohort IIB (n = 10) | Mean | 230.0 | 36.4 | 6.5 | 4.5 | 5314.2 | 78.7 | 10.5 | 23.6 | 143.2 |
| ≥6 to <12 y | SD | 58.7 | 11.4 | 0.9 | 4.2 | 2842.6 | 68.9 | 3.5 | 8.9 | 131.9 |
| Chewable tablet | Median | 225.0 | 35.1 | 6.2 | 2.9 | 4524.0 | 43.4 | 10.5 | 23.4 | 108.8 |
| CV% | 25.5 | 31.3. | 13.4 | 93.5 | 53.3 | 87.6 | 33.6 | 37.7 | 92.1 | |
| GM | 223.0 | 34.8 | 6.4 | 3.4 | 4660.6 | 57.6 | 10.0 | 22.2 | 110.3 | |
| Cohort III (n = 12) | Mean | 89.6 | 14.2 | 6.2 | 4.1 | 5204.8 | 39.5 | 9.5 | 13.3 | 71.3 |
| 2 to <6 y | SD | 22.5 | 2.2 | 0.7 | 3.2 | 2940.6 | 21.9 | 5.5 | 10.1 | 57.0 |
| Chewable tablet | Median | 75.0 | 13.4 | 6.1 | 3.1 | 5143.5 | 35.8 | 7.3 | 10.3 | 67.8 |
| CV% | 25.1 | 15.7 | 10.7 | 78.5 | 56.5 | 55.5 | 58.6 | 76.1 | 80.0 | |
| GM | 87.5 | 14.1 | 6.2 | 3.3 | 4328.6 | 31.6 | 8.0 | 11.0 | 52.0 |
Abbreviations: AUC12, area under the concentration-time curve from 0 to 12 hours postdose; C12, concentration at 12 hours postdose; CL/F, oral clearance; Cmax, maximum concentration; CV%, percent coefficient of variation; GM, geometric mean; L/h, liters per hour; SD, standard deviation; T1/2, half-life; V/F, oral volume of distribution.