A pharmacokinetic comparison of cyclosporin oral solution and cyclosporin capsules in heart and lung transplant recipients.
Pharmacokinetic profiles were obtained for 16 heart or lung recipients following the administration of identical doses of cyclosporin as oral solution and capsules on consecutive days. A comparison of pharmacokinetic parameters (AUC, Cmax, Cmin and tmax) showed that there were no significant differences between the two formulations except for the tmax, which was significantly longer for the capsules. The mean variation in day-to-day trough levels produced by the two different forms was 25.6%. A retrospective study was carried out of consecutive cyclosporin levels in patients at steady state on oral solution. The mean variation in day-to-day trough levels was 32.3%. This was not significantly different from the variation in consecutive trough levels seen in the oral solution/capsule comparison. This study shows that cyclosporin capsules can be substituted for oral solution without causing acute changes in cyclosporin blood levels, and that the pharmacokinetics of the two formulations are similar.
Eadon
H
H
Department of Pharmacy, Harefield Hospital, Middlesex, UK.
Rose
M
M
O'Neill
R
R
Leaver
N
N
Yacoub
M
M
D000284:Administration, Oral; D002214:Capsules; D016572:Cyclosporine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005260:Female; D006084:Graft Rejection / Q000188:drug therapy / Q000378:metabolism; D006207:Half-Life; D016027:Heart Transplantation; D006801:Humans; D016040:Lung Transplantation; D008297:Male; D008875:Middle Aged; D012189:Retrospective Studies
D002214:Capsules; D016572:Cyclosporine