Geometric mean (95% confidence interval) of casopitant, M13, and total radioactivity plasma pharmacokinetic parameters after single-dose i.v. (target dose: 90 mg) and oral (target dose: 150 mg) administration of [14C]casopitant to humans
Parameter | Intravenous | Oral | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Casopitant | M13 | Total Radioactivity | Casopitant | M13 | Total Radioactivity | |||||
| n | 6 | 6 | 6 | 6 | 6 | 6 | ||||
| AUC(0-∞) (ng/h/ml)a | 6980 | 2940 | 101000 | 6620 | 5620 | 183,000 | ||||
| (5490, 8890) | (2110, 4100) | (69,700, 148,000) | (3640, 12,100) | (3610, 8760) | (161,000, 208,000) | |||||
| AUC(0-t) (ng/h/ml)a | 6730 | 2720 | 37,900 | 6240 | 5160 | 81,700 | ||||
| (5330, 8500) | (1990, 3710) | (32,100, 44,800) | (3570, 10,900) | (3690, 7230) | (72,000, 92,600) | |||||
| Cmax (ng/ml)a | 2080 | 110 | 228 | 761 | 297 | 2160 | ||||
| (1700, 2560) | (97.1, 124) | (1810, 2870) | (509, 1140) | (250, 352) | (1970, 2360) | |||||
| tmax (h)b | 0.25 | 3.50 | 0.25 | 1.00 | 2.02 | 2.50 | ||||
| (0.25, 0.25) | (0.50, 4.00) | (0.25, 0.25) | (0.50, 2.00) | (1.00, 4.00) | (1.00, 4.00) | |||||
| t1/2 (h) | 15.6 | 16.9 | 107 | 17.0 | 17.4 | 78.6 | ||||
| (11.2, 21.8) | (11.9, 24.1) | (74.9, 153) | (11.5, 25.1) | (11.0, 27.5) | (68.0, 91.0) | |||||
| CL (l/h) | 12.9 | 0.887 | ||||||||
| (10.1, 16.4) | (0.610, 1.29) | |||||||||
| Vdss (liter) | 194 | 136 | ||||||||
|
| (156, 240) |
| (114, 162) |
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