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Pharmacokinetic Evaluation of a New Oral Cyclosporine Formulation
Author(s) -
Whipple Julianne K.,
Lewis Kelly S.,
Weitman Steven D.,
Ausman Robert K.,
Bourne David WA.,
Andrews Walter,
Adams Mark B.,
Sasse Edward A.,
Quebbeman Edward J.
Publication year - 1994
Publication title -
pharmacotherapy: the journal of human pharmacology and drug therapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.227
H-Index - 109
eISSN - 1875-9114
pISSN - 0277-0008
DOI - 10.1002/j.1875-9114.1994.tb02794.x
Subject(s) - medicine , pharmacokinetics , bioavailability , crossover study , regimen , oral administration , dosing , pharmacology , surgery , placebo , alternative medicine , pathology
Study Objective . To compare the pharmacokinetics of a new oral cyclosporine preparation with those of cyclosporine solution diluted in Isocal and the intravenous formulation. Design . Randomized, crossover trial. Setting . Tertiary care referral center. Patients . Seven pediatric liver 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 intravenous and oral dosage forms. Patients received one dose of intravenous cyclosporine, and then were randomized to receive their usual oral cyclosporine dose incorporated into a chocolate wafer or mixed with Isocal. After a minimum of 3 days, the alternative preparation was administered. Serial cyclosporine blood samples were collected at predetermined intervals for 12 hours after the third dose for each regimen. Concentrations 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 seen in F, k a , C max , and Wax between the two oral cyclosporine preparations (p>0.05). No new rejection episodes occurred during the study period. Conclusions . We conclude there is no difference in the bioavailability of the oral solution and the chocolate formulation. We believe the new preparation may increase patient compliance and ensure administration of a complete dose compared with the currently marketed solution.