PHARMACOKINETIC EVALUATION OF A NEW ORAL CYCLOSPORINE FORMULATION

Study Objective. To compare the pharmacokinetics of a new oral cyclosp orine preparation with those of cyclosporine solution diluted in Isoca l and the intravenous formulation. Design. Randomized, crossover trial . Setting. Tertiary care referral center. Patients. Seven pediatric li ver transplant recipients who were receiving oral cyclosporine as part of their immunosuppressive regimen. All. patients completed the study . Interventions. Pharmacokinetic studies were performed with the intra venous and oral dosage forms. Patients received one dose of intravenou s cyclosporine, and then were randomized to receive their usual oral c yclosporine dose incorporated into a chocolate wafer or mixed with Iso cal. After a minimum of 3 days, the alternative preparation was admini stered. Serial cyclosporine blood samples were collected at predetermi ned intervals for 12 hours after the third dose for each regimen. Conc entrations were determined by high-performance liquid chromatography. The data for the three dosage forms were fit simultaneously with a two -compartment model. Measurements and Main Results. No difference was s een in F, k(a), C-max, and t(max) between the two oral cyclosporine pr eparations (p>0.05). No new rejection episodes occurred during the stu dy period. Conclusions. We conclude there is no difference in the bioa vailability of the oral solution and the chocolate formulation. We bel ieve the new preparation may increase patient compliance and ensure ad ministration of a complete dose compared with the currently marketed s olution.