Modelling Ciclosporin Double-Peak Absorption Profiles in the Early Post-Transplantation Period

Authors: Annick Rousseau1; Pierre Marquet1

Source: Clinical Pharmacokinetics, Volume 43, Number 14, 2004 , pp. 1055-1057(3)

Publisher: Adis International

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Abstract:

Objective: To apply a recent double-peak absorption model to ciclosporin.

Methods: Pharmacokinetic evaluation was performed in 20 patients who had undergone de novo renal transplantation and were receiving immunosuppressive therapy with corticosteroids, mycophenolate mofetil and ciclosporin Neoral®. Data were analysed by nonlinear mixed-effects modelling using individual and population approaches.

Results: Six patients presented pharmacokinetic profiles with two peaks, whereas 14 curves apparently had a single, sometimes delayed and wide, peak. A one-compartment model with first-order elimination in association with the double-peak absorption model best fitted the data. This model reliably described the pharmacokinetics of ciclosporin, whether or not a double peak was present on the concentration-time profiles.

Conclusions: The double-peak absorption model could be useful to optimise ciclosporin exposure in the early post-transplantation period.

Keywords: Immunosuppressants, pharmacokinetics; Ciclosporin, pharmacokinetics; Renal transplant

Document Type: Research article

Affiliations: 1: Department of Pharmacology and Toxicology, University Hospital, Limoges, France

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