title: Single dose pharmacokinetics of ciclosporin and its main metabolites after oral ciclosporin as oily solution or capsule.
abstract: The commercially available oily solution of ciclosporin which has to be suspended before intake is disliked by some patients for bad taste and has a variable bioavailability. In this investigation the oral pharmacokinetics of ciclosporin and its main metabolites 1 and 17 of the oily solution (Sandimmun) and a soft gelatine capsule preparation of ciclosporin were compared in a crossover fashion in 10 kidney allograft recipients. The results demonstrate a bioequivalence of both formulations. In either case metabolite 17 had a significantly longer half-life than either ciclosporin or metabolite 1. At earlier time-points the concentration of ciclosporin could be best correlated with metabolite 1 and at later time-points with metabolite 17. Both metabolites were less correlated with each other in the late absorption phase of ciclosporin.
authors.affiliation: Abteilung Allgemeine Pharmakologie, Medizinische Hochschule Hannover, Fed. Rep. of Germany.
authors.forename: J S
authors.initials: JS
authors.lastname: Bleck
authors.forename: B
authors.initials: B
authors.lastname: Nashan
authors.forename: U
authors.initials: U
authors.lastname: Christians
authors.forename: R
authors.initials: R
authors.lastname: Schottmann
authors.forename: K
authors.initials: K
authors.lastname: Wonigeit
authors.forename: K F
authors.initials: KF
authors.lastname: Sewing
mesh_terms: D000328:Adult; D002214:Capsules; D002851:Chromatography, High Pressure Liquid; D003524:Cyclosporins / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D005260:Female; D006207:Half-Life; D006801:Humans; D016030:Kidney Transplantation / Q000276:immunology; D008297:Male; D008875:Middle Aged; D009821:Oils; D011863:Radioimmunoassay; D012996:Solutions
chemical_list: D002214:Capsules; D003524:Cyclosporins; D009821:Oils; D012996:Solutions