The Effect of Drug Formulation on the Pharmacokinetics of Cyclosporine.

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The effect of dosage form on the pharmacokinetics of cyclosporine (CYA) in steady state after oral administration as either a capsule or a solution was studied in 4 renal trans plant recipients. CYA (dose; 100-350mg/day) was administered orally to the patients (17-49 years old) every 12 hr. The whole blood levels were measured by fluorescence polarization immu noassay (FPIA) based on monoclonal antibody. The blood specimens were collected just before administration (0h) in the morning and at1 (1h), 2 (2h), (3h), 6 (6h), 8 (8h) hours after administration; specimens were also collected just before the evening administration (12h) and at1 (13h), 2 (14h), 3 (15h), 4 (16h), 7 (19h), 12 (24h) hours after administration in one day. There were no significant differences between capsule and solution the administrations in the area-under-the-curve (AUC), and in the maximal blood concentration (Cmax). There was a significant difference between the trough level of 0h and 24h, and between the time of maximum blood concentration (Tmax) after the administration of solution in the daytime and that at nighttime (p<0.05). These results suggest that the capsule is not only as applicable as solution in changeover patients but also very useful for trough blood level monitoring.
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