Study on pharmacokinetics and bioavailability of domestic cyclosporin A microemulsion capsule

Objective: To compare the pharmacokinetics and the relative bioavailability of a domestic cyclosporin A (CsA) microemulsion capsule and an imported one. Methods: A single oral dose of New Cyspin (NO capsule or Neoral (Neo) capsule was given to 10 healthy volunteers in a randomized crossover study. Drug concentrations in blood were determined by fluorescence polarization immunoassay. The data were dealt with 3P87 pharmacokinetics program. Results:The concentration-time curve of CsA conformed to first-order absorption and 2 compartment model. The t1/2β, tmax and cmax of NC capsule were (4. 89±1. 84) h,(1. 89 ± 0. 41) h and (875. 26±168. 63) ng · ml-1, respectively, and of Neo capsule were (4. 78± 1. 49) h,(1. 96 ± 0. 32) h and (908. 48±167. 23) ng · ml-1 .respectively. The bioavailability of NC capsule was (96. 47± 8. 69)% of Neo capsule. Conclusion: The pharmacokinetics and bioavailability of NC capsule have no significant differences from those of Neo capsule. NC capsule and Neo capsule are bioequivalent.