S. Takahara et al., A COMPARATIVE-STUDY OF FK506 GRANULES AND CAPSULES IN RENAL-TRANSPLANT RECIPIENTS, Transplant international, 11(3), 1998, pp. 181-185
Nine renal transplant recipients in stable systemic condition on FK506
capsules were converted to FK506 granules in order to investigate the
safety, efficacy, and pharmacokinetics of the granular formulation of
FK506. The study period for the administration of FK506 granules was
4 weeks, and in principle, the oral dose was the same as that of the F
K506 capsules. Renal graft function remained stable and no rejection s
igns were noticed while the patients were taking the granules. The are
a under the blood concentration-time curve (AUC), the maximum blood le
vel (C-max), and the time to reach C-max (T-max) after FK506 capsules
and FK506 granules were, respectively, 93.1 +/- 66.4 and 97.0 +/- 89.1
ng . h/ml (P = 0.81), 12.7 +/- 7.1 and 15.2 +/- 11.7 ng/ml (P = 0.39)
, and 2.0 +/- 1.7 and 1.3 +/- 0.6 h (P = 0.29). The mean trough blood
level during FK506 medication was 4.25 +/- 3.42 and 4.02 +/- 3.83 ng/m
l, respectively, for the capsules and the granules. FK506 granules, a
new formulation, showed an efficacy comparable to that of the FK506 ca
psular formulation.