与健康志愿者静脉注射14C-溴化地斯的明相比，单次口服地斯的明后的绝对生物利用度、药代动力学、肾脏和胆汁清除率。
Absolute bioavailability, pharmacokinetics, renal and biliary clearance of distigmine after a single oral dose in comparison to i.v. administration of 14C-distigmine-bromide in healthy volunteers.
作者信息
Vree T B, Waitzinger J, Hammermaier A, Radhofer-Welte S
机构信息
Institute of Anesthesiology, Academic Hospital Nijmegen, The Netherlands.
出版信息
Int J Clin Pharmacol Ther. 1999 Aug;37(8):393-403.
AIM
The aim of the study was to determine the absolute bioavailability and pharmacokinetics after a single dose oral administration in comparison to i.v. administration of 14C-labelled distigmine-bromide (14C-Ubretid) in healthy male volunteers.
RESULTS
After the intravenous administration, distigmine is eliminated from the body by renal excretion (85%), and for a small fraction by biliary excretion in the feces (4%). This situation is reversed after an oral administration, where 6.5% of the dose is recovered from the urine and 88% from the feces. This means that distigmine after oral administration is hardly absorbed, the calculated bioavailability is 4.65%.
CONCLUSION
The mean absorption time (MAT) after oral administration was 10 h, influencing the t(1/2alpha) (1.4 vs 4.5 h) and the t(1/2beta) (60 vs 70 h) to higher values than after the i.v. administration (p < 0.05).
目的
本研究的目的是在健康男性志愿者中，与静脉注射14C标记的溴化地斯的明（14C-Ubretid）相比，确定单次口服给药后的绝对生物利用度和药代动力学。
结果
静脉给药后，地斯的明通过肾脏排泄从体内消除（85%），一小部分通过胆汁排泄到粪便中（4%）。口服给药后情况相反，剂量的6.5%从尿液中回收，88%从粪便中回收。这意味着口服给药后地斯的明几乎不被吸收，计算得出的生物利用度为4.65%。
结论
口服给药后的平均吸收时间（MAT）为10小时，与静脉给药后相比，使t(1/2α)（1.4对4.5小时）和t(1/2β)（60对70小时）升高至更高值（p < 0.05）。
Zotero 插件