Absorption characteristics of EC-MPS--an enteric-coated formulation of mycophenolic sodium.

Enteric-coated mycophenolate sodium is an advanced formulation delivering mycophenolic acid (MPA), designed to improve MPA-related upper gastrointestinal adverse events by delaying MPA release until the small intestine. Objective: Two studies were undertaken to identify the absolute bioavailability and dose-proportionality of enteric-coated mycophenolate sodium in stable renal transplant patients receiving cyclosporine. Methods: Study 1: The mean MPA AUC 0-t was shown to be greater after MPA infusion than after oral enteric-coated mycophenolate sodium (42.1 vs. 28.9 μg × h/ml). Mean absolute bioavailability was 0.71 ± 0.21 (SD). Study 2: The AUC 0-t and C max for MPA were proportional to the dose of enteric-coated mycophenolate sodium, similarly mean AUC 0-∞ and C max for MPA glucuronide were proportional to dose administered. Results and conclusions: In patients receiving cyclosporine the absolute bioavailability of MPA provided by enteric-coated mycophenolate sodium is equivalent to that provided by mycophenolate mofetil when administered in combination with cyclosporine, and exhibits dose-proportionality. Enteric-coated mycophenolate sodium was well tolerated from 180 - 2,160 mg with no serious adverse events reported.