Bleck J S, Nashan B, Christians U, Schottmann R, Wonigeit K, Sewing K F
Abteilung Allgemeine Pharmakologie, Medizinische Hochschule Hannover, Fed. Rep. of Germany.
Arzneimittelforschung. 1990 Jan;40(1):62-4.
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.
市售的环孢素油溶液在服用前必须混悬，一些患者因味道不佳而不喜欢它，并且其生物利用度可变。在本研究中，以交叉方式比较了10例肾移植受者中环孢素油溶液（山地明）及其主要代谢物1和17以及环孢素软胶囊制剂的口服药代动力学。结果表明两种制剂具有生物等效性。在任何一种情况下，代谢物17的半衰期均明显长于环孢素或代谢物1。在较早的时间点，环孢素的浓度与代谢物1的相关性最好，而在较晚的时间点与代谢物17的相关性最好。在环孢素的吸收后期，两种代谢物之间的相关性较低。
