Decreased oral availability of cyclosporin A at second administration in humans

Br J Clin Pharmacol. 1997 Oct;44(4):343-5. doi: 10.1046/j.1365-2125.1997.t01-1-00599.x.

Abstract

Aims: The objective of this study was to determine the extent of period effect on the pharmacokinetics of cyclosporin A (CsA) during consecutive dosing.

Methods: Sandimmune Neoral and Neoplanta capsules were administered to twenty-four healthy Korean male subjects at a single CsA dose of 175 mg in a 2 x 2 crossover investigation with a 2-week wash-out phase. Concentrations of CsA in blood were measured by a r.i.a. method for a period of 48 h.

Results: The two formulations were found bioequivalent, but analysis of variance (ANOVA) indicated that there is a significant (P < 0.01) period effect in AUC(0,last) (area under the blood concentration-time curve above the assay limit) and Cmax (maximum blood concentration) between the administrations. A 6 and 9% decrease in the AUC(0,last) and Cmax, respectively was seen at the second administration.

Conclusions: This period effect on the pharmacokinetics of CsA may be relevant for the patients who need consecutive administration of the drug.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Adult
  • Area Under Curve
  • Biological Availability
  • Cyclosporine / administration & dosage
  • Cyclosporine / pharmacokinetics*
  • Humans
  • Immunosuppressive Agents / administration & dosage
  • Immunosuppressive Agents / pharmacokinetics*
  • Male
  • Metabolic Clearance Rate
  • Therapeutic Equivalency

Substances

  • Immunosuppressive Agents
  • Cyclosporine