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Keywords:

  • Cyclosporine;
  • IntralipidTM;
  • Pharmacokinetics

Abstract

The effect of IntralipidTM co-administration on the pharmacokinetics of cyclosporine (CyA) was studied in NZW rabbits. A single intravenous bolus dose of CyA (10 mg kg−1) 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 (t1/2) of CyA was significantly lower with Intralipid administration (191·25 min) than control (298 ± 59 min). The total body clearance (C1TOT) and volume of distribution (Vdss) 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 0·05 ± 0·01 and 0·17 ± 0·06, respectively. Co-administration of Intralipid with CyA decreased both the ClTOT and Vdss resulting in a rapid elimination, i.e., decrease in a t1/2 of CyA from the body.