Effect of co-administration of intralipidTM on the pharmacokinetics of cyclosporine in the rabbit

✍ Scribed by Ajit K. Shah; Ronald J. Sawchuk

• Publisher: John Wiley and Sons
• Year: 1991
• Tongue: English
• Weight: 498 KB
• Volume: 12
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/bdd.2510120607

✦ Synopsis

The effect of IntralipidTM co-administration on the pharmacokinetics of cyclosporine (CyA) was studied in NZW rabbits. A single intravenous bolus dose of CyA (10mg kg-') mixed with 3 ml of Intralipid was administered to rabbits (n = 4). Control animals (n = 4) received the same dose of CyA without Intralipid. Serial blood samples were collected up to 12 h after the administration of CyA. Concentrations of CyA in plasma were analyzed using a HPLC method. The terminal elimination half-life (t,) of CyA was significantly lower with Intralipid administration (191 f 25 min) than control (298 f 59 min). The total body clearance (ClToT) and volume of distribution (Vd,) of CyA was reduced by approximately 65-70 per cent with Intralipid administration compared to control. The free fraction of CyA in plasma with and without Intralipid administration was estimated to be 005 f 001 and 0.17 f 0.06, respectively. Co-administration of Intralipid with CyA decreased both the ClTOT and Vd,, resulting in a rapid elimination, i.e., decrease in a t, of CyA from the body.