Absorption characteristics of a microemulsion formulation of cyclosporine in de novo pediatric liver transplant recipients.

摘要: In pediatric liver transplant recipients, oral cyclosporine (CsA) therapy may be complicated by impaired or delayed absorption during the initial weeks posttransplant. Neoral (NL) is a microemulsion preconcentrate formulation of CsA expected to increase rate and extent have less pharmacokinetic variability. The absolute bioavailability (F) from NL was compared with that currently marketed Sandimmune (SM) in double-blind, crossover study conducted 9 recipients (age 6 months 11 years) between 8 20 days After determination pharmacokinetics for steady-state intravenous dose, patients were randomized receive single dose SM period I alternative II. Clearance (Clt) volume distribution (Vss) values (mean±s.d.) calculated i.v. similar previously reported (Clt=12.0±1.3 ml/min/kg ; Vss=2.2±0.2 L/kg). Mean F (±SD) significantly higher than (NL=37.6±14.6% SM=24.7±8.0% P=0.05). Although not reaching statistical significance, observed maximum blood concentration (Cmax) higher, time Cmax (Tmax) shorter patients. There no significant correlations age any parameter group as whole-however, there statistically (r=0.87 P=0.02), Vss (r=0.91 P=0.01) aged 2 years less. this population, demonstrated improved (% F) Sandimmune. less, function and/or bowel length.