Pharmacokinetic parameters of SAC, NAc-SAC, SACS, and NAc-SACS in rats after oral and i.v. administration
Data represent mean ± S.D. of three to four rats
| Parameters | SACa | NAc-SACa | SACSa | NAc-SACSa | |
|---|---|---|---|---|---|
| i.v. | Oral | i.v. | i.v. | i.v. | |
| Cmax (mg/l) | 6.2 ± 0.56 | 3.9 ± 0.64 | 13 ± 2.7 | 15 ± 1.8 | 14 ± 1.7 |
| tmax (h) | — | 0.27 ± 0.17 | — | — | — |
| t1/2 (h) | 1.1 ± 0.27 | 1.2 ± 0.19 | 1.0 ± 0.25 | 0.99 ± 0.13 | 0.84 ± 0.41 |
| CL (l/h/kg) | 0.91 ± 0.035 | — | 1.8 ± 0.34 | 1.5 ± 0.13 | 1.3 ± 0.19 |
| CLr (l/h/kg) | 0.0086 | — | 1.5 | 0.0014 | 1.2 |
| Vss (l/kg) | 1.0 ± 0.072 | — | 0.94 ± 0.21 | 0.75 ± 0.056 | 0.45 ± 0.028 |
| Bioavailability (%) | — | 92.1 | — | — | — |
| AUC (mg·l/h) | |||||
| SAC | 5.50 ± 0.21 | 5.07 ± 0.58 | 1.87 ± 0.33 | n.d. | n.d. |
| NAc-SAC | 1.80 ± 0.19 | 1.96 ± 0.39 | 2.89 ± 0.66 | n.d. | n.d. |
| SACS | 0.057 ± 0.013 | 0.062 ± 0.014 | n.d. | 3.47 ± 0.32 | n.d. |
| NAc-SACS | 0.11 ± 0.025 | 0.11 ± 0.013 | 0.13 ± 0.073 | 1.29 ± 0.090 | 4.05 ± 0.64 |
| GSAC | 0.063 ± 0.011 | 0.059 ± 0.011 | 0.010 ± 0.001 | n.d. | n.d. |
n.d., not detected; tmax, time to reach Cmax; Vss, distribution volume at steady state.
↵a A single oral or i.v. dose (5 mg/kg) of SAC, NAc-SAC, SACS, and NAc-SACS was administered to rats.