Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2005, 149(2):309-313 | DOI: 10.5507/bp.2005.048

PHARMACOKINETIC CONVERSION STUDY OF A NEW CYCLOSPORINE FORMULATION IN STABLE ADULT RENAL TRANSPLANT RECIPIENTS

František Perlík^a, Marwan A. Masri^b, M. Rost^c, Vojtěch Kamarád^d

^a Institute of Pharmacology, 1st Faculty of Medicine, Charles University, Prague, Czech Republic

^b Rizk Hospital, Beirut, Lebanon

^c Univerity of South Bohemia, České Budějovice, Czech Republic

^d Clinical Department R&D, IVAX-CR, a.s., Opava, Czech Republic

Cyclosporine A (CyA) is a standard component of immunosuppressive regimens. It is a critical-dose drug for which a minor change in absorption can have important clinical consequences. The aim of the study was to compare the pharmacokinetics and safety of the new generic CyA formulation, Equoral® capsules, after a switch from original formulation, Neoral® capsules, in seventy stable adult renal transplant recipients. The extent and rate of pharmacokinetic parameters for bioequivalence were compared in a non-randomized, steady-state clinical study with fixed non-replicate study design. Pharmacokinetic analysis of CyA have shown that both the rate and extent of absorption of Equoral® does not differ significantly from that of Neoral®. At identical dosing, the new formulation was found to have geometric means of C_max 717 ng/ml and AUCτ 3108 ng/ml.h, while corresponding results of comparator were 725 ng/ml and AUCτ 3039 ng/ml.h, respectively. The 90 % confidence intervals of C_max and AUCτ were within 80- 125 % interval of the mean values. The results suggest that Equoral® capsules can be used as an alternative treatment to Neoral® capsules in CyA regimen.

Keywords: Cyclosporine A, Comparative study Equoral vs. Neoral, Bioequivalence

Received: October 6, 2005; Accepted: November 30, 2005; Published: December 1, 2005  Show citation