Biotransformations of oxaliplatin in rat blood in vitro

✍ Scribed by Feng R. Luo; Steven D. Wyrick; Stephen G. Chaney

• Book ID: 101270914
• Publisher: John Wiley and Sons
• Year: 1999
• Tongue: English
• Weight: 208 KB
• Volume: 13
• Category: Article
• ISSN: 1095-6670
• DOI: 10.1002/(sici)1099-0461(1999)13:3/4<159::aid-jbt6>3.0.co;2-c

✦ Synopsis

The partitioning and biotransformations of oxaliplatin 1 [trans-l-1,2-diaminocyclohexaneoxalatoplatinum(II)] were investigated in the blood of Wistar male rats in vitro. [3-H]-Oxaliplatin was incubated with rat blood at 37ЊC in 5% CO 2 and the concentrations of all Pt complexes containing the [3-H]-dach carrier ligand were followed for up to 12 hours. Decay for both oxaliplatin and Pt-dach 2 in the plasma ultrafiltrate (PUF) was rapid (t 1/2 oxaliplatin 0.68 h and t 1/2 for Pt-dach in the PUF 0.85 h). After 9 hours, the concentration of oxaliplatin fell below the detection limit. By 4 hours, the PUF-Pt-dach reached a plateau, which was 12% of total Pt-dach. The binding of Pt-dach to red blood cells (RBCs) and plasma proteins was also very rapid (t 1/2 RBCs 0.58 h and t 1/2 plasma proteins 0.78 h) and reached equilibrium by 4 hours. At equilibrium, 35% of total Pt-dach was bound to plasma proteins, 12% was in the plasma ultrafiltrate, and 53% was found as-