Aj. Amante et al., A PHARMACOKINETIC COMPARISON OF THE CORN-OIL VERSUS MICROEMULSION GELCAP FORMULATION OF CYCLOSPORINE USED DE-NOVO AFTER RENAL-TRANSPLANTATION, Transplant international, 10(3), 1997, pp. 217-222
The initial poor absorption of the corn oil-based, gel capsule oral fo
rmulation of cyclosporin (CyA) greatly limits its use for inception of
immunosuppressive therapy. Insufficient drug concentrations during th
e early post-transplant period predispose to renal allograft rejection
. The present study served to compare the time required to achieve the
rapeutic CyA concentrations after de novo administration of the corn o
il-based gel capsule (CyA-GC; n = 11) versus the microemulsion (CyA-ME
; n = 11) formulation of CyA. During the Ist month after renal transpl
antation, patients underwent serial pharmacokinetic profiling from whi
ch we obtained observed and dose-corrected values of several parameter
s. Although patients in neither the CyA-GC nor the CyA-ME group adequa
tely absorbed the drug during days 0-2, from day 3 to 4 patients in th
e CyA-ME group showed significantly greater absorption than those in t
he CyA-GC group (P = 0.041). Patients in the CyA-ME group reached the
Ist month target average concentration (C-av) values (greater than or
equal to 550 ng/ml) earlier than those in the CyA-GC group and require
d significantly lower dally CyA doses (P = 0.018). We conclude that th
erapeutic CyA levels can be achieved more rapidly and with lower doses
of the drug after de novo administration of CyA-ME than with CyA-GC.