Pharmacokinetic parameters of paliperidone and total radioactivity in plasma
Data are mean ± S.D. [except for tmax: median (minimum—maximum)] obtained from healthy male subjects (n = 5) receiving a 1-mg single oral dose of [14C]paliperidone.
| Parameter | Total Radioactivity [14C] | Paliperidone |
|---|---|---|
| Cmax (ng/ml)a | 9.54 ± 1.35 | 8.85 ± 1.31 |
| tmax (h) | 1.5 (1.0-1.5) | 1.5 (1.0-1.5) |
| AUC24 h (ng · h/ml)a | 114 ± 19.9 | 111 ± 22.0 |
| AUC∞ (ng · h/ml)a | 175 ± 30.7 | 187 ± 29.3 |
| t1/2 (h) | 15.2 ± 2.15 | 24.8 ± 4.35 |
| CL/f (ml/min) | 97.9 ± 17.6 | 91.0 ± 15.0 |
| Ae0-168 h (% dose) | ||
| Urine | 79.6 ± 4.20 | 59.4 ± 7.12 |
| Feces | 11.4 ± 3.07 | Not detected |
| CLCR (ml/min) | 113 ± 10.3 | |
| CLR (ml/min) | 53.1 ± 9.47 | |
| CLGFR (ml/min)b | 25.9 ± 2.36 | |
| CLact (ml/min) | 27.2 ± 7.50 |
Cmax, maximum peak plasma concentration; tmax, time to maximum peak plasma concentration; AUC24 h, area under the plasma concentration-time curve from 0 to 24 h; AUC∞, area under the plasma concentration-time curve from zero to infinity; t1/2, terminal half-life; CL/f, total plasma clearance; Ae (% dose), amount of unchanged drug excreted in the urine/feces; CLCR, creatinine clearance; CLR, renal clearance; CLGFR, average clearance by glomerular filtration rate; CLac, active renal clearance.
↵ a For total radioactivity, the units for Cmax and AUC were nanogram-equivalents per milliliter and nanogram-equivalents per milliliter per hour per milliliter, respectively.
↵ b For the calculation of clearance by glomerular filtration (CLGFR), the fraction unbound of paliperidone was 0.23.