Table 3.
Predicted plasma and lung tissue exposure under different dosage regimens of chloroquine phosphate.
| No. | Dosage design | Visual population (default models in Simcyp) | Plasma |
Lung (mean value of five lobes) |
||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Cmax (ng/mL) | AUC (h·μg/mL) |
Ctrough (μg/mL) |
AUC (h·μg/mL) |
|||||||||
| 0–120 h | 0–240 h | Day 1 (24 h) | Day 3 (72 h) | Day 5 (120 h) | Day 7 (168 h) | Day 10 (240 h) | 0–120 h | 0–240 h | ||||
| A | Day 1: 1000 mg, 500 mg Days 2–3: 500 mg QD |
Chinese healthy volunteers | 215 | 17.3 | 27.4 | 10.5 | 29.0 | 39.4 | 45.9 | 51.2 | 2760 | 8350 |
| B | Days 1–10: 500 mg QD | Chinese healthy volunteers | 283 | 13.6 | 38.7 | 3.79 | 16.0 | 32.0 | 50.6 | 81.1 | 1690 | 8450 |
| C | Days 1–7: 500 mg BID | Chinese healthy volunteers | 416 | 25.5 | 63.1 | 6.21 | 29.2 | 60.6 | 97.2 | 129 | 3020 | 15,100 |
| D | Day 1: 750 mg BID Days 2–5: 500 mg BID |
Chinese healthy volunteers | 364 | 29.2 | 54.9 | 9.32 | 35.6 | 68.8 | 90.2 | 108 | 3650 | 14,700 |
| E | Day 1: 750 mg, 500 mg Days 2–3: 500 mg BID Days 4–5: 250 mg BID |
Chinese healthy volunteers | 270 | 23.9 | 43.1 | 8.65 | 32.8 | 56.7 | 71.8 | 84.1 | 3220 | 12,000 |
| F | Days 1–5: 250 mg BID | Chinese healthy volunteers | 172 | 12.5 | 24.4 | 3.11 | 14.6 | 30.3 | 40.4 | 48.6 | 1510 | 6470 |