Table 1 Mean pharmacokinetic parameters (± standard deviation) of tofacitinib after its intravenous administration at a dose of 10 mg/kg to CON, LGN, AKI, and AKI-LGN rats
| Parameters | CON ( |
LGN ( |
AKI ( |
AKI-LGN ( |
|---|---|---|---|---|
| Body weight (g) | 292 ± 12.2 | 268 ± 10.9 | 181 ± 3.91 |
243 ± 17.0 |
| Terminal half-life (min) | 46.0 ± 12.0 | 28.0 ± 11.7 | 154 ± 65.8 |
61.1 ± 16.0 |
| AUC (µg∙min/mL) | 243 ± 22.0 | 257 ± 13.1 | 788 ± 128 |
249 ± 36.6 |
| CL (mL/min/kg) | 41.4 ± 3.64 | 39.0 ± 1.99 | 13.0 ± 1.93 |
42.5 ± 4.18 |
| CLR (mL/min/kg) | 2.17 ± 0.284 | 2.25 ± 0.892 | 0.0741 ± 0.0629 |
1.42 ± 0.358 |
| CLNR (mL/min/kg) | 39.3 ± 3.45 | 36.8 ± 2.23 | 12.9 ± 1.89 |
41.7 ± 4.45 |
| Vss (mL/kg) | 880 ± 405 | 490 ± 84.0 | 889 ± 475 | 1585 ± 346 |
| Ae0-24 h (% of dose) | 5.24 ± 0.524 | 5.79 ± 2.37 | 0.536 ± 0.424 | 2.65 ± 1.61 |
| GI24 h (% of dose) | 0.0393 ± 0.0241 | 0.165 ± 0.139 | 0.419 ± 0.296 | 0.0303 ± 0.00232 |
Ae0-24 h, the amount of tofacitinib excreted in the urine over 24 h; AKI, acute kidney injury; AKI-LGN, acute kedney injury-logaini; AUC, area under plasma concentration-time curves from time zero to time infinity; CL, time-averaged total body clearance; CLNR, time-averaged non-renal clearance; CLR, time-averaged renal clearance; CON, control; GI24 h, the percentage of drug remaining in the gastrointestinal tract at 24 h; LGN, loganin; Vss, the apparent volume of distribution at steady state. *AKI is significantly different (