Table 4.
Pharmacokinetic Parameters of OP in Rats After IV Injection of OP and Oral Administration of OP-S or ODSF with Various Levels of OP
| Test Material | OP | OP-S | ODSF (2.5) | ODSF (10) | ODSF (20) |
|---|---|---|---|---|---|
| Administration route | IV | Oral | Oral | Oral | Oral |
| Dose of OP (mg/kg) | 5 | 10 | 2.5 | 10 | 20 |
| Tmax (h) | - | 0.5±0.0 | 0.5±0.0 | 0.5±0.0 | 0.5±0.0 |
| Cmax (μg/mL) | 2.29±0.418 | 0.071±0.006 | 0.049±0.003 | 0.136±0.016 | 0.224±0.055 |
| AUClast (μg·h/mL) | 7.44±0.832 | 0.965±0.038 | 0.894±0.024 | 1.62±0.125 | 2.52±0.460 |
| AUCinf (μg·h/mL) | 11.6±1.58 | 3.52±1.75 | 3.44±1.94 | 2.99±0.352 | 4.49±0.666 |
| Bioavailability (%) | 100 | 6.48±0.252 | 24.0±0.642 | 10.9±0.838 | 8.47±1.55 |
Notes: Each value is mean±standard deviation (n=4). Bioavailability (%): (AUClast, oral/DoseOP, oral)/(AUClast, IV/DoseOP, IV)×100.
Abbreviations: OP, oxaliplatin; IV, intravenous; OP-S, OP in aqueous solution; DLM, Nα-deoxycholyl-l-lysyl-methylester; OP/DLM, ion-pairing complex between OP and DLM; P188, poloxamer 188; ODSF, solid oral formulation of OP/DLM with P188 and Labrasol; Tmax, time to reach maximum plasma concentration; T1/2, half-life of plasma concentration; Cmax, maximum plasma concentration; AUClast, area under the plasma concentration–time curve from zero to the time of the last measurable plasma concentration; AUCinf, area under the plasma concentration–time curve from zero to infinity.