Heidemann R, Gracien E, Menke G, Rietbrock N
Dtsch Med Wochenschr. 1987 May 1;112(18):719-22. doi: 10.1055/s-2008-1068127.
In a randomized crossover study on twelve healthy test subjects, the plasma concentration of isosorbide-5-nitrate (IS-5-N) after oral administration of 40 mg IS-5-N daily from two standard preparations (two tablets Ismo 20 or Corangin 20) and two sustained release preparations with 40 mg or 60 mg IS-5-N (one tablet Corangin 40 or Corangin 60) once a day was determined. The concentrations were measured in the first and in the third dose interval (24 hours). The respective pharmacokinetic parameters (AUC, Cmax and tmax) of the first and the third day only differed slightly. The two standard formulations proved to be bioequivalent. With the two sustained release preparations, maximum plasma concentrations attained after five to six hours were measured which were lower by roughly the factor 2. The sustained release preparations showed a low loss of bioavailability of 13-19% as compared to the nonretarded standard formulations.
在一项针对12名健康受试者的随机交叉研究中,测定了每日口服40毫克5-单硝酸异山梨酯(IS-5-N)后,两种标准制剂(两片20毫克易顺脉或20毫克长效心痛治)和两种含40毫克或60毫克IS-5-N的缓释制剂(一片40毫克长效心痛治或60毫克长效心痛治)的血浆IS-5-N浓度。在第一个和第三个给药间隔(24小时)测量浓度。第一天和第三天各自的药代动力学参数(AUC、Cmax和tmax)仅有轻微差异。两种标准制剂被证明具有生物等效性。对于两种缓释制剂,在五到六个小时后测得的最大血浆浓度比标准制剂低约2倍。与非缓释标准制剂相比,缓释制剂的生物利用度损失较低,为13%-19%。