Eadon H, Rose M, O'Neill R, Leaver N, Yacoub M
Department of Pharmacy, Harefield Hospital, Middlesex, UK.
Transpl Int. 1995;8(1):35-40. doi: 10.1007/BF00366708.
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.
连续两天给16名心脏或肺移植受者服用相同剂量的环孢素口服溶液和胶囊后，获得了药代动力学曲线。药代动力学参数（AUC、Cmax、Cmin和tmax）的比较表明，除tmax外，两种制剂之间无显著差异，胶囊的tmax明显更长。两种不同剂型产生的每日谷浓度平均变化为25.6%。对服用口服溶液处于稳态的患者的连续环孢素水平进行了回顾性研究。每日谷浓度的平均变化为32.3%。这与口服溶液/胶囊比较中连续谷浓度的变化无显著差异。该研究表明，环孢素胶囊可替代口服溶液，而不会引起环孢素血药浓度的急性变化，且两种制剂的药代动力学相似。
