Pharmacokinetic parameters of MRL-A in rats and dogs
Rats and dogs were dosed intravenously with a solution of the hydrochloride salt in ethanol/PEG 400/saline (20:40:40) or orally with a suspension of the hydrochloride salt in 20% ethanol/80% methylcellulose (0.5% w/v). Data are listed as the mean ± standard deviation.
Dose | AUC0-∞ | CLp | Vdss |
t 1/2 |
| μM · h | ml/min/kg | l/kg | h | |
| i.v. | ||||
| Rats (n = 4) | ||||
| 0.5 mg/kg | 0.9 ± 0.1 | 20.3 ± 1.0 | 10.6 ± 0.6 | 6.8 ± 0.7 |
| Dogs (n = 3) | ||||
| 0.5 mg/kg | 6.2 ± 1.4 | 3.1 ± 0.7 | 2.0 ± 0.2 | 10.0 ± 0.2 |
|
| AUC0-∞ |
C
max
|
T
max
| F |
| μM · h | μM | h | % | |
| Oral | ||||
| Rats (n = 4) | ||||
| 1 mg/kg | 1.5 ± 0.5 | 0.1 ± 0.0 | 5.0 ± 1.2 | 83 |
| Dogs (n = 3) | ||||
| 1 mg/kg | 10.7 ± 3.3 | 1.0 ± 0.3 | 2.0 ± 0.0 | 86a |
↵ a Bioavailability of 1 mg/kg dose in dogs was determined individually for each dog in a crossover experiment with the same dogs dosed intravenously at 0.5 mg/kg.