Table 2.
Pharmacokinetic parameters for ARTS and DHA following i.v. and i.m. ARTS ( 120 mg (312.5 µmol); Group 1 and i.v. ARTS ( 120 mg (312.5 µmol) followed by rectal DHA ( 563 µmol (160 mg); Group 2. Data are given as mean ±s.d. unless otherwise indicated.
| Intravenous ARTS (n = 11) | Intramuscular ARTS (n = 11) | |||
|---|---|---|---|---|
| Group 1 | ARTS | DHA | ARTS | DHA |
| Dose (µmol kg−1) | 5.7±0.8 | – | 5.7±0.8 | – |
| t1/2 (min) | 3.2±2.1 | 59±23 | 41±18 | 64±21 |
| MRT (min) | 4.1±1.2 | 83±28 | 59±29 | 114±22 |
| CL (l h−1 kg−1) | 2.8±1.5 | 0.64±0.22 | 2.9±1.2c | 0.73±0.21c |
| V (l kg−1) | 0.22±0.16 | 0.8±0.2 | 2.6±1.2c | 1.1±0.4c |
| AUC (µmol l−1 h) | 2.7±1.4 | 10.1±4.0 | 2.6±1.9 | 8.7±3.4 |
| Cmax (µm) | 42±24a | 9.7 (7.7–12.0)b | 2.3 (2.0–4.8)b | 4.1 (3.2–4.6)b |
| tmax (min) | – | 7.0 (5.5–11.2)b | 12 (10–15)b | 45 (34–60)b |
| Bioavailability | – | – | – | 0.88±0.19 |
| Intravenous ARTS (n = 12) | Rectal DHA (n = 11d) | ||
|---|---|---|---|
| Group 2 | ARTS | DHA | DHA |
| Dose (µmol kg−1) | 5.9±0.5 | – | 10.7±1.0 |
| t1/2 (min) | 4.4±0.8 | 50±12 | – |
| CL (l h−1 kg−1) | 2.1±0.8 | 0.48±0.14 | – |
| V (l kg−1) | 0.22±0.12 | 0.55±0.12 | – |
| AUC (µmol l−1 h) | 3.2±1.1 | 11.6±4.1 | 3.4±1.3e |
| Cmax (µm) | 43±16a | 9.6 (8.8–14.0)b | 0.75 (0.55–1.11)b |
| tmax (min) | – | 9 (8–13.5)b | 240 (158–360)b |
| Bioavailability (%) | – | – | 16 (13–25)b |
a
Value extrapolated to the end of the 2 min i.v. ARTS injection.
b
Median (interquartile range).
c
Apparent clearance (CL/F) and apparent volume of distribution (V/F).
d
Inadequate data obtained from one patient.
e
AUC(0,8 h).