Okolicsanyi L, Venuti M, Orlando R, Lirussi F, Nassuato G, Benvenuti C
Int J Clin Pharmacol Ther Toxicol. 1982 Oct;20(10):482-7.
The bioavailability of p.o. and i.v. cimetidine was studied in 12 patients with compensated liver cirrhosis in a crossover study. Single doses of 200 and 400 mg cimetidine were used for both administration routes. Plasma concentration and urinary recovery were determined by the HPLC method. The pharmacokinetic data observed in these patients do not differ from those of normal subjects and patients. A positive correlation between AUC and cimetidine oral dose was found. Oral bioavailability of cimetidine was about 94% compared to that of the i.v. route. The p.o. dose of 400 mg produced AUC values similar to the i.v. dose of 400 mg. After 400 mg cimetidine p.o. the mean peak plasma level was higher and the time for which plasma levels remained above 0.5 mg/l was longer. There were no significant differences between plasma cimetidine levels after the intravenous administration of 200 and 400 mg. The urinary recovery of cimetidine was significantly higher after intravenous administration independently of the given dose. The pharmacokinetics of cimetidine does not appear to be altered in liver cirrhosis.
在一项交叉研究中，对12例代偿期肝硬化患者口服和静脉注射西咪替丁的生物利用度进行了研究。两种给药途径均使用单剂量200毫克和400毫克西咪替丁。采用高效液相色谱法测定血浆浓度和尿回收率。在这些患者中观察到的药代动力学数据与正常受试者和患者的数据无差异。发现AUC与西咪替丁口服剂量之间呈正相关。与静脉注射途径相比，西咪替丁的口服生物利用度约为94%。400毫克的口服剂量产生的AUC值与400毫克的静脉注射剂量相似。口服400毫克西咪替丁后，平均血浆峰值水平更高，血浆水平保持在0.5毫克/升以上的时间更长。静脉注射200毫克和400毫克后，血浆西咪替丁水平无显著差异。无论给予何种剂量，静脉注射后西咪替丁的尿回收率均显著更高。肝硬化患者中西咪替丁的药代动力学似乎未发生改变。
